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  1. Fulltext Design, synthesis and biological potential of heterocyclic benzoxazole scaffolds as promising antimicrobial and anticancer agents
    Kakkar S, Kumar S, Narasimhan B, Lim SM, Ramasamy K, Mani V, et al.
    Chem Cent J, 2018 Sep 19;12(1):96.
    PMID: 30232633 DOI: 10.1186/s13065-018-0464-8
    BACKGROUND: Benzoxazole is the most important class of heterocyclic compound in medicinal chemistry. It has been incorporated in many medicinal compounds making it a versatile heterocyclic compound that possess a wide spectrum of biological activities.

    RESULTS: The molecular structures of synthesized benzoxazole derivatives were confirmed by physicochemical and spectral means. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity against selected microbial species using tube dilution method and antiproliferative activity against human colorectal carcinoma (HCT 116) cancer cell line by Sulforhodamine B assay.

    CONCLUSION: In vitro antimicrobial results demonstrated that compounds 4, 5, 7 and 16 showed promising antimicrobial potential. The in vitro anticancer activity indicated that compounds 4 and 16 showed promising anticancer activity against human colorectal cancer cell line (HCT 116) when compared to standard drug and these compounds may serve as lead compound for further development of novel antimicrobial and anticancer agents.

  2. Exploration of synthetic multifunctional amides as new therapeutic agents for Alzheimer's disease through enzyme inhibition, chemoinformatic properties, molecular docking and dynamic simulation insights
    Hassan M, Abbasi MA, Aziz-Ur-Rehman, Siddiqui SZ, Hussain G, Shah SAA, et al.
    J Theor Biol, 2018 12 07;458:169-183.
    PMID: 30243565 DOI: 10.1016/j.jtbi.2018.09.018
    A new series of multifunctional amides has been synthesized having moderate enzyme inhibitory potentials and mild cytotoxicity. 2-Furyl(1-piperazinyl)methanone (1) was coupled with 3,5-dichloro-2-hydroxybenzenesulfonyl chloride (2) to form {4-[(3,5-dichloro-2-hydroxyphenyl)sulfonyl]-1-piperazinyl}(2-furyl)methanone (3). Different elecrophiles were synthesized by the reaction of various un/substituted anilines (4a-o) with 2-bromoacetylbromide (5), 2‑bromo‑N-(un/substituted-phenyl)acetamides (6a-o). Further, equimolar ratios of 3 and 6a-o were allowed to react in the presence of K2CO3 in acetonitrile to form desired multifunctional amides (7a-o). The structural confirmation of all the synthesized compounds was carried out by their EI-MS, IR, 1H NMR and 13C NMR spectral data. Enzyme inhibition activity was performed against acetyl and butyrylcholinestrase enzymes, whereby 7e showed very good activity having IC50 value of 5.54 ± 0.03 and 9.15 ± 0.01 μM, respectively, relative to eserine, a reference standard. Hemolytic activity of the molecules was checked to asertain their cytotoxicity towards red blood cell membrance and it was observed that most of the compounds were not toxic up to certain range. Moreover, chemoinformatic protepties and docking simulation results also showed the significance of 7e as compared to other compounds. Based on in vitro and in silico analysis 7e could be used as a template for the development of new drugs against Alzheimer's disease.
  3. The influences of age, gender and geometric pattern of visual image on the verticality perception: A subjective visual vertical (SVV) study among Malaysian adults
    Zakaria MN, Salim R, Tahir A, Zainun Z, Mohd Sakeri NS
    Clin Otolaryngol, 2019 03;44(2):166-171.
    PMID: 30411501 DOI: 10.1111/coa.13255
    OBJECTIVES: Subjective visual vertical (SVV) is a simple, quick and reliable test for measuring utricular function. The literature on the effects of fundamental demographic variables such as age and gender on SVV is inconclusive and should be supported by research with larger samples. The aim of the present study was to determine the influences of age, gender and geometric pattern of visual image on SVV among healthy adults.

    STUDY DESIGN: This study employed a repeated measures design.

    SETTINGS: Otorhinolaryngology Clinic, Hospital Universiti Sains Malaysia, Malaysia.

    PARTICIPANTS: Eligible Malaysian adults (N = 187, aged 21-75 years) were recruited and categorised into young (N = 60), middle-aged (N = 66) and older (N = 61) groups. Most of them were Malay, and 51.3% were men.

    MAIN OUTCOME MEASURES: Subjective visual vertical angles (in degrees) were determined from each participant in a static upright condition using a computerised SVV device. They were asked to indicate their verticality perception for three types of visual images (solid line, dotted line and arrow pattern).

    RESULTS: Three-way mixed ANOVA revealed insignificant influences of age and gender on SVV results (P > 0.05). In contrast, mean SVV angles were significantly higher for the arrow pattern than for other visual images (P = 0.004).

    CONCLUSION: While the insignificant influences of age and gender on static SVV are further ascertained with larger samples, the perception of verticality is less accurate when aligning a more geometrically complex visual image (ie, arrow pattern). Further SVV research on vestibular-disordered patients is beneficial, particularly to verify the normative data obtained with this complex visual image.

  4. Fulltext Synthesis, biological evaluation and corrosion inhibition studies of transition metal complexes of Schiff base
    Kashyap S, Kumar S, Ramasamy K, Lim SM, Shah SAA, Om H, et al.
    Chem Cent J, 2018 Nov 20;12(1):117.
    PMID: 30460466 DOI: 10.1186/s13065-018-0487-1
    BACKGROUND: The transition metal complexes formed from Schiff base is regarded as leading molecules in medicinal chemistry. Because of the preparative availability and diversity in the structure of central group, the transition metals are important in coordination chemistry. In the present work, we have designed and prepared Schiff base and its metal complexes (MC1-MC4) and screened them for antimicrobial, anticancer and corrosion inhibitory properties.

    METHODOLOGY: The synthesized metal complexes were characterized by physicochemical and spectral investigation (UV, IR, 1H and 13C-NMR) and were further evaluated for their antimicrobial (tube dilution) and anticancer (SRB assay) activities. In addition, the corrosion inhibition potential was determined by electrochemical impedance spectroscopy (EIS) technique.

    RESULTS AND DISCUSSION: Antimicrobial screening results found complexes (MC1-MC4) to exhibit less antibacterial activity against the tested bacterial species compared to ofloxacin while the complex MC1 exhibited greater antifungal activity than the fluconazole. The anticancer activity results found the synthesized Schiff base and its metal complexes to elicit poor cytotoxic activity than the standard drug (5-fluorouracil) against HCT116 cancer cell line. Metal complex MC2 showed more corrosion inhibition efficiency with high Rct values and low Cdl values.

    CONCLUSION: From the results, we can conclude that complexes MC1 and MC2 may be used as potent antimicrobial and anticorrosion agents, respectively.

  5. Fulltext Design, synthesis and biological evaluation of 3-(2-aminooxazol-5-yl)-2H-chromen-2-one derivatives
    Kakkar S, Kumar S, Lim SM, Ramasamy K, Mani V, Shah SAA, et al.
    Chem Cent J, 2018 Dec 04;12(1):130.
    PMID: 30515643 DOI: 10.1186/s13065-018-0499-x
    BACKGROUND: In view of wide range of biological activities of oxazole, a new series of oxazole analogues was synthesized and its chemical structures were confirmed by spectral data (Proton/Carbon-NMR, IR, MS etc.). The synthesized oxazole derivatives were screened for their antimicrobial and antiproliferative activities.

    RESULTS AND DISCUSSION: The antimicrobial activity was performed against selected fungal and bacterial strains using tube dilution method. The antiproliferative potential was evaluated against human colorectal carcinoma (HCT116) and oestrogen- positive human breast carcinoma (MCF7) cancer cell lines using Sulforhodamine B assay and, results were compared to standard drugs, 5-fluorouracil and tamoxifen, respectively.

    CONCLUSION: The performed antimicrobial activity indicated that compounds 3, 5, 6, 8 and 14 showed promising activity against selected microbial species. Antiproliferative screening found compound 14 to be the most potent compound against HCT116 (IC50 = 71.8 µM), whereas Compound 6 was the most potent against MCF7 (IC50 = 74.1 µM). Further, the molecular docking study has been carried to find out the interaction between active oxazole compounds with CDK8 (HCT116) and ER-α (MCF7) proteins indicated that compound 14 and 6 showed good dock score with better potency within the ATP binding pocket and may be used as a lead for rational drug designing of the anticancer molecule.

  6. Synthesis of some new N-(alkyl/aralkyl)-N-(4-methoxyphenethyl) benzene sulfonamides as antibacterial agents against Escherichia
    Abbasi MA, Fatima Z, Rehman AU, Siddiqui SZ, Ali Shah SA, Shahid M, et al.
    Pak J Pharm Sci, 2019 Sep;32(5):1957-1964.
    PMID: 31813858
    The present study comprises the synthesis of a new series of benzenesulfonamides derived from N-sulfonation of 2-(4-methoxyphenyl)-1-ethanamine (1). The synthesis was initiated by the reaction of 2-(4-methoxyphenyl)-1-ethanamine (1) with benzenesulfonyl chloride (2), to yield N-(4-methoxyphenethyl)benzenesulfonamide (3). This parent molecule 3 was subsequently treated with various alkyl/aralkyl halides (4a-j) in N,N-dimethylformamide (DMF) and in the presence of a weak base lithium hydride (LiH) to obtain various N-(alkyl/aralkyl)-N-(4-methoxyphenethyl) benzenesulfonamides (5a-j). The characterization of these derivatives was carried out by spectroscopic techniques like IR, 1H-NMR, and 13C-NMR. Elemental analysis also supported this data. The biofilm inhibitory action of all the synthesized compounds was carried out on Escherichia coli and some of the compounds were identified to be very suitable inhibitors of this bacterial strain. Furthermore, the molecules were also tested for their cytotoxicity behavior to assess their utility as less cytotoxic therapeutic agents.
  7. Antidiabetic and antidyslipidemic potential of Echinops echinatus in rat models of type I and type II diabetes
    Chaudhry SRY, Akram A, Aslam N, Wajid M, Iqbal Z, Nazir I, et al.
    Pak J Pharm Sci, 2019 Mar;32(2):505-514.
    PMID: 31081759
    Echinops echinatus is traditionally an important plant that finds its extensive use as a diuretic, anti-inflammatory, anti-pyretic, nerve tonic, abortifacient, aphrodisiac, antiasthmatic, and antidiabetic agent. The current study investigates protection against the hyperglycemia and dyslipidemia in alloxan-induced (type I diabetes) and fructose-fed insulin resistance (type II diabetes) models of diabetes treated with aqueous methanolic root extract of E. echinatus (Ee.Cr). Albino rats were treated orally with Ee.Cr at doses 100, 300 and 500mg/kg. The fasting blood glucose was measured by glucometer, while standard kits were used to determine the levels of serum total cholesterol, triglycerides and HDL. The administration of Ee.Cr significantly (P<0.001) reduced the FBG concentration in a dose-dependent pattern in alloxan-induced and fructose-fed diabetic rats. The Ee.Cr also corrected the dyslipidemia associated with fructose and alloxan-induced diabetes by significantly (P<0.001) decreasing the concentration of serum total cholesterol, triglycerides, and LDL and by increasing HDL concentration. Ee.Cr also significantly (P<0.001) improved the glucose tolerance in fructose-fed rats. We conclude that Ee.Cr has antidiabetic and antidyslipidemic effects in both insulin-dependent alloxan-induced diabetes and fructose-induced insulin resistance diabetes rat models.
  8. Experimental data on glucose and energy levels of orange mud crab, Scylla olivacea at different water velocities
    Taufik M, Amin-Safwan A, Mohd Nordin AR, Shahrul I, Abol-Munafi AB, Ikhwanuddin M
    Data Brief, 2020 Apr;29:105232.
    PMID: 32099875 DOI: 10.1016/j.dib.2020.105232
    The present datasets were conducted to investigate glucose concentration in hemolymph, energy levels at selected body parts (hepatopancreas, muscle, gonad), and feces among different sexes of crabs cultured at four different water velocities (0, 20, 40, and 60 cm/s) during a 60-day culture period. A total of 102 immature crabs (51 males, and 51 females) were sampled from Kuala Muda, Kedah coastal water, Peninsular Malaysia (5°39'N 100°19'E) from April to November of 2018. Results indicated that glucose concentration was the highest at water velocity of 60 cm/s for both male and female crabs (♂: 3.76 ± 0.08 mmol/L; ♀: 3.63 ± 0.06 mmol/L), whereas at 0 cm/s, the lowest levels of glucose concentration (♂: 0.13 ± 0.08 mmol/L; ♀: 0.19 ± 0.06 mmol/L) were recorded. As for energy analysis in hepatopancreas, results showed that both male and female crabs recorded the highest levels at 0 cm/s (no flow) with 37.919 ± 0.07 KJ/g and 34.636 ± 0.50 KJ/g, respectively. Energy for locomotion (muscle) of male crabs recorded the highest at 0 cm/s (♂: 26.823 ± 0.06 KJ/g), meanwhile for females, the highest was recorded at 20 cm/s (26.607 ± 0.34 KJ/g). Energy for reproduction of males could not be compared due to an insufficient available amount of testes/vas deferens, whereas female crabs recorded the highest energy usage at 20 cm/s water velocity (♀: 37.895 ± 0.08 KJ/g). For feces, both male and female crabs recorded the lowest energy at 60 cm/s (♂: 5.841 ± 0.03 KJ/g; ♀: 5.393 ± 0.01 KJ/g). Glucose assessment showed a direct relationship between increased velocity and glucose secretion in hemolymph at high velocity of 60 cm/s (stress condition) compared to other treatments. Regarding energy analysis, this research improved the mechanism of hepatopancreas, gonad, muscle and feces functions in development and reproduction, while it shed light on the influence of velocity on energy metabolism of S. olivacea.
  9. Synthesis, Bacterial biofilm inhibition and cytotoxicity of new N-Alkyl/aralkyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-nitrobenzenesulfonamides
    Abbasi MA, Zeb A, Rehman A, Siddiqui SZ, Shah SAA, Shahid M, et al.
    Pak J Pharm Sci, 2020 Jan;33(1):41-47.
    PMID: 32122829
    The current research was commenced by reaction of 1,4-benzodioxane-6-amine (1) with 4-nitrobenzenesulfonyl chloride (2) in the presence of aqueous base under dynamic pH control at 9 to yield N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-nitrobenzenesulfonamide (3) which was further reacted with a series of alkyl/aralkyl halides (4a-i) in polar aprotic solvent using catalytic amount of lithium hydride which acts as base to afford some new N-alkyl/aralkyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-nitrobenzenesulfonamides (5a-i). The projected structures of all the synthesized derivatives were characterized by contemporary techniques i.e., IR, 1H-NMR and EIMS. The biofilm Inhibitory action of all synthesized molecules was carried out against Escherichia coli and Bacillus subtilis. It was inferred from their results that 5f and 5e exhibited suitable inhibitory action against the biofilms of these bacterial strains. Moreover, their cytotoxicity was also checked and it was concluded that these synthesized molecules displayed docile cytotoxicity.
  10. Synthesis, spectral analysis and biological evaluation of sulfamoyl and 1,3,4-oxadiazole derivatives of 3-pipecoline
    Rehman A, Aslam SJ, Abbasi MA, Siddiqui SZ, Rasool S, Shah SAA
    Pak J Pharm Sci, 2019 May;32(3):987-996.
    PMID: 31278711
    Heterocyclic chemistry is an important field of organic chemistry due to therapeutic potential. The minor modification in the structure of poly-functional compounds has great effect on therapeutic ability. In the presented research work, substituted 1,3,4-oxadiazole derivatives, 8a-p, have been synthesized by the reaction of 1-(4-bromomethylbenzenesulfonyl)-3-methylpiperidine (7) and 5-substituted-1,3,4-oxadiazole-2-thiol (4a-p). The 5-substituted-1,3,4-oxadiazole-2-thiol were synthesized by converting carboxylic acids correspondingly into esters, hydrazides and oxadiazoles. Secondly the electrophile, 1-(4-Bromomethylbenzenesulfonyl)-3-methylpiperidine (7), was prepared by the reaction of 3-methylpiperidine with 4-bromomethylbenzenesulfonyl chloride in the presence of water and Na2CO3 under pH of 9-10. The compounds were structurally corroborated through spectroscopic data analysis of IR, EI-MS and 1H-NMR. The screening for antibacterial activity revealed the compounds to be moderate to excellent inhibitors against bacteria under study. Anti-enzymatic activity was assessed against urease enzyme and 1-{[4-({[5-(3-nitrophenyl)-1,3,4-oxadiazol-2-yl]sulfanyl}methyl)phenyl]sulfonyl}-3-methylpiperidine (8d) was the most active one.
  11. Green synthesis of selenium-N-heterocyclic carbene compounds: Evaluation of antimicrobial and anticancer potential
    Kamal A, Nazari V M, Yaseen M, Iqbal MA, Ahamed MBK, Majid ASA, et al.
    Bioorg Chem, 2019 09;90:103042.
    PMID: 31226469 DOI: 10.1016/j.bioorg.2019.103042
    Three benzimidazolium salts (III-V) and respective selenium adducts (VI-VIII) were designed, synthesized and characterized by various analytical techniques (FT-IR and NMR 1H, 13C). Selected salts and respective selenium N-Heterocyclic carbenes (selenium-NHC) adducts were tested in vitro against Cervical Cancer Cell line (Hela), Breast Adenocarcinoma cell line (MCF-7), Retinal Ganglion Cell line (RGC-5) and Mouse Melanoma Cell line (B16F10) using MTT assay and the results were compared with standard drug 5-Fluorouracil. Se-NHC compounds and azolium salts showed significant anticancer potential. Molecular docking studies of compounds (VI, VII and VIII) showed strong binding energies and ligand affinity toward following angiogenic factors: VEGF-A (vascular endothelial growth factor A), EGF (human epidermal growth factor), HIF (Hypoxia-inducible factor) and COX-1 (Cyclooxygenase-1) suggesting that the anticancer activity of adducts (VI, VII and VIII) may be due to their strong anti-angiogenic effect. In addition, compounds III-VIII were screened for their antibacterial and antifungal potential. Adduct VI was found to be potent anti-fungal agent against A. Niger with zone of inhibition (ZI) value 27.01 ± 0.251 mm which is better than standard drug Clotrimazole tested in parallel.
  12. Fulltext Oxygen-Releasing Antibacterial Nanofibrous Scaffolds for Tissue Engineering Applications
    Abudula T, Gauthaman K, Hammad AH, Joshi Navare K, Alshahrie AA, Bencherif SA, et al.
    Polymers (Basel), 2020 May 29;12(6).
    PMID: 32485817 DOI: 10.3390/polym12061233
    Lack of suitable auto/allografts has been delaying surgical interventions for the treatment of numerous disorders and has also caused a serious threat to public health. Tissue engineering could be one of the best alternatives to solve this issue. However, deficiency of oxygen supply in the wounded and implanted engineered tissues, caused by circulatory problems and insufficient angiogenesis, has been a rate-limiting step in translation of tissue-engineered grafts. To address this issue, we designed oxygen-releasing electrospun composite scaffolds, based on a previously developed hybrid polymeric matrix composed of poly(glycerol sebacate) (PGS) and poly(ε-caprolactone) (PCL). By performing ball-milling, we were able to embed a large percent of calcium peroxide (CP) nanoparticles into the PGS/PCL nanofibers able to generate oxygen. The composite scaffold exhibited a smooth fiber structure, while providing sustainable oxygen release for several days to a week, and significantly improved cell metabolic activity due to alleviation of hypoxic environment around primary bone-marrow-derived mesenchymal stem cells (BM-MSCs). Moreover, the composite scaffolds also showed good antibacterial performance. In conjunction to other improved features, such as degradation behavior, the developed scaffolds are promising biomaterials for various tissue-engineering and wound-healing applications.
  13. Synthesis, Characterization, Antimicrobial and Anticancer Studies of Metal Complexes of 2-methoxy-4-((3-methylpyridin-2-ylimino)methyl)phenol
    Mishra A, Tahlan S, Ramasamy K, Lim SM, Shah SAA, Narasimhan B
    Mini Rev Med Chem, 2020;20(13):1311-1317.
    PMID: 32368977 DOI: 10.2174/1389557520666200505124125
    BACKGROUND: Being derived from primary amine and aromatic aldehyde, Schiff base and their complexes have an imperative role in the improvement of inorganic chemistry, which are broadly studied as coordination compounds and are gradually becoming more important in biochemical and analytical applications.

    METHODS: They have also been used for antibacterial, antifungal, anticancer, antitubercular activities. Novel synthesised Schiff's base 2-methoxy-4-((3-methylpyridin-2-ylimino)methyl)phenol (SB) and its metal complexes (Zn[II], Cu[II], Co[II] and Ni[II]) were characterised by UV, IR and NMR spectroscopy. Formation of the Schiff base and the metal (Zn[II], Cu[II], Co[II] and Ni[II]) chelates was supported by spectral and analytical data. The ligand and metal complexes have been screened for their antibacterial activity against Staphylococcus aureus, Salmonella typhi, Escherichia coli, Klebsiella pneumoniae and antifungal activity against the fungi Candida albicans and Aspergillus niger. Further, the synthesised compounds were also screened for antiproliferative activity against the human colorectal carcinoma (HCT116) cell line using the Sulforhodamine B assay.

    RESULT: Metal complexes formed were found to enhance the potency of the Schiff base due to coordination with a copper complex, showing better activity than others.

    CONCLUSION: Copper complex was observed to be more potent than other complexes against all the pathogenic microbes and cancer cell line (HCT116).

  14. Fulltext Strengthening Primary Health-Care Services to Help Prevent and Control Long-Term (Chronic) Non-Communicable Diseases in Low- and Middle-Income Countries
    Haque M, Islam T, Rahman NAA, McKimm J, Abdullah A, Dhingra S
    Risk Manag Healthc Policy, 2020;13:409-426.
    PMID: 32547272 DOI: 10.2147/RMHP.S239074
    The prevalence of long-term (chronic) non-communicable diseases (NCDs) is increasing globally due to an ageing global population, urbanization, changes in lifestyles, and inequitable access to healthcare. Although previously more common in high- and upper-middle-income countries, lower-middle-income countries (LMICs) are more affected, with NCDs in LMICs currently accounting for 85-90% of premature deaths among 30-69 years old. NCDs have both high morbidity and mortality and high treatment costs, not only for the diseases themselves but also for their complications. Primary health care (PHC) services are a vital component in the prevention and control of long-term NCDs, particularly in LMICs, where the health infrastructure and hospital services may be under strain. Drawing from published studies, this review analyses how PHC services can be utilized and strengthened to help prevent and control long-term NCDs in LMICs. The review finds that a PHC service approach, which deals with health in a comprehensive way, including the promotion, prevention, and control of diseases, can be useful in both high and low resource settings. Further, a PHC based approach also provides opportunities for communities to better access appropriate healthcare, which ensures more significant equity, efficiency, effectiveness, safety, and timeliness, empowers service users, and helps healthcare providers to achieve better health outcomes at lower costs.
  15. Fulltext Movie Review Summarization Using Supervised Learning and Graph-Based Ranking Algorithm
    Khan A, Gul MA, Zareei M, Biswal RR, Zeb A, Naeem M, et al.
    Comput Intell Neurosci, 2020;2020:7526580.
    PMID: 32565772 DOI: 10.1155/2020/7526580
    With the growing information on web, online movie review is becoming a significant information resource for Internet users. However, online users post thousands of movie reviews on daily basis and it is hard for them to manually summarize the reviews. Movie review mining and summarization is one of the challenging tasks in natural language processing. Therefore, an automatic approach is desirable to summarize the lengthy movie reviews, and it will allow users to quickly recognize the positive and negative aspects of a movie. This study employs a feature extraction technique called bag of words (BoW) to extract features from movie reviews and represent the reviews as a vector space model or feature vector. The next phase uses Naïve Bayes machine learning algorithm to classify the movie reviews (represented as feature vector) into positive and negative. Next, an undirected weighted graph is constructed from the pairwise semantic similarities between classified review sentences in such a way that the graph nodes represent review sentences, while the edges of graph indicate semantic similarity weight. The weighted graph-based ranking algorithm (WGRA) is applied to compute the rank score for each review sentence in the graph. Finally, the top ranked sentences (graph nodes) are chosen based on highest rank scores to produce the extractive summary. Experimental results reveal that the proposed approach is superior to other state-of-the-art approaches.
  16. The influence of type of visual image and gender on the perception of horizontality: a subjective visual horizontal (SVH) study
    Zakaria MN, Tahir A, Zainun Z, Salim R, Mohd Sakeri NS, Abdul Wahat NH
    Acta Otolaryngol, 2021 Jan;141(1):62-65.
    PMID: 32957810 DOI: 10.1080/00016489.2020.1817552
    BACKGROUND: The graviceptive otolith function can be measured using subjective visual horizontal (SVH) testing. Nevertheless, more research efforts are required to understand the essential variables affecting SVH.

    OBJECTIVE: The aim of the present study was to determine the effects of type of visual image and gender on subjective visual horizontal (SVH) perception among healthy adults.

    MATERIALS AND METHODS: In this comparative study, 50 healthy young adults were enrolled. While in an upright body position, they were required to report their perception of horizontality for two types of visual images (solid line and arrow pattern) using a computerized SVH device.

    RESULTS: The arrow pattern produced significantly bigger SVH angles than the solid line (p < .001). In contrast, no significant influence of gender was found on SVH results (p = .743), Based on the statistical outcomes, the preliminary normative data for SVH were established.

    CONCLUSIONS AND SIGNIFICANCE: The arrow pattern (a more complex visual image) produced bigger SVH deviations than the simple solid line image. In contrast, the horizontality perception does not appear to be affected by gender. The preliminary normative SVH data gathered from the present study can be beneficial for clinical and future research applications.

  17. REPORT - Synthesis of promising antibacterial and antifungal agents: 2-[[(4-Chlorophenyl)sulfonyl](2,3-dihydro-1,4-benzodioxin-6-yl)amino]-N-(un/substituted-phenyl)acetamides
    Abbasi MA, Irshad M, Aziz-Ur-Rehman -, Siddiqui SZ, Nazir M, Ali Shah SA, et al.
    Pak J Pharm Sci, 2020 Sep;33(5):2161-2170.
    PMID: 33824125
    In the presented work, 2,3-dihydro-1,4-benzodioxin-6-amine (1) was reacted with 4-chlorobenzenesulfonyl chloride (2) in presence of aqueous basic aqueous medium to obtain 4-chloro-N-(2,3-dihydro-1,4-benzodioxin-6-yl)benzenesulfonamide (3). In parallel, various un/substituted anilines (4a-l) were treated with bromoacetyl bromide (5) in basified aqueous medium to obtain corresponding 2-bromo-N-(un/substituted)phenylacetamides (6a-l) as electrophiles. Then the compound 3 was finally reacted with these electrophiles, 6a-l, in dimethylformamide (DMF) as solvent and lithium hydride as base and activator to synthesize a variety of 2-[[(4-chlorophenyl)sulfonyl](2,3-dihydro-1,4-benzodioxin-6-yl)amino]-N-(un/substituted)phenylacetamides (7a-l). The synthesized compounds were corroborated by IR, 1H-NMR and EI-MS spectral data for structural confirmations. These molecules were then evaluated for their antimicrobial and antifungal activities along with their %age hemolytic activity. Some compounds were found to have suitable antibacterial and antifungal potential, especially the compound 2-[[(4-chlorophenyl)sulfonyl](2,3-dihydro-1,4-benzodioxin-6-yl)amino]-N-(3,5-dimethylphenyl)acetamide (7l) exhibited good antimicrobial potential with low value of % hemolytic activity.
  18. Fulltext Comparing insertion characteristics on nasogastric tube placement by using GlideScope™ visualization vs. MacIntosh laryngoscope assistance in anaesthetized and intubated patients
    Wan Ibadullah WH, Yahya N, Ghazali SS, Kamaruzaman E, Yong LC, Dan A, et al.
    Braz J Anesthesiol, 2016 Jul-Aug;66(4):363-8.
    PMID: 27343785 DOI: 10.1016/j.bjane.2014.11.013
    BACKGROUND AND OBJECTIVE: This was a prospective, randomized clinical study to compare the success rate of nasogastric tube insertion by using GlideScope™ visualization versus direct MacIntosh laryngoscope assistance in anesthetized and intubated patients.

    METHODS: Ninety-six ASA I or II patients, aged 18-70 years were recruited and randomized into two groups using either technique. The time taken from insertion of the nasogastric tube from the nostril until the calculated length of tube had been inserted was recorded. The success rate of nasogastric tube insertion was evaluated in terms of successful insertion in the first attempt. Complications associated with the insertion techniques were recorded.

    RESULTS: The results showed success rates of 74.5% in the GlideScope™ Group as compared to 58.3% in the MacIntosh Group (p=0.10). For the failed attempts, the nasogastric tube was successfully inserted in all cases using rescue techniques. The duration taken in the first attempt for both techniques was not statistically significant; Group A was 17.2±9.3s as compared to Group B, with a duration of 18.9±13.0s (p=0.57). A total of 33 patients developed complications during insertion of the nasogastric tube, 39.4% in Group A and 60.6% in Group B (p=0.15). The most common complications, which occurred, were coiling, followed by bleeding and kinking.

    CONCLUSION: This study showed that using the GlideScope™ to facilitate nasogastric tube insertion was comparable to the use of the MacIntosh laryngoscope in terms of successful rate of insertion and complications.
  19. Fulltext Multitargeted Molecular Docking and Dynamic Simulation Studies of Bioactive Compounds from Rosmarinus officinalis against Alzheimer's Disease
    Mirza FJ, Zahid S, Amber S, Sumera, Jabeen H, Asim N, et al.
    Molecules, 2022 Oct 25;27(21).
    PMID: 36364071 DOI: 10.3390/molecules27217241
    Alzheimer's disease (AD) has been associated with the hallmark features of cholinergic dysfunction, amyloid beta (Aβ) aggregation and impaired synaptic transmission, which makes the associated proteins, such as β-site amyloid precursor protein cleaving enzyme 1 (BACE I), acetylcholine esterase (AChE) and synapsin I, II and III, major targets for therapeutic intervention. The present study investigated the therapeutic potential of three major phytochemicals of Rosmarinus officinalis, ursolic acid (UA), rosmarinic acid (RA) and carnosic acid (CA), based on their binding affinity with AD-associated proteins. Detailed docking studies were conducted using AutoDock vina followed by molecular dynamic (MD) simulations using Amber 20. The docking analysis of the selected molecules showed the binding energies of their interaction with the target proteins, while MD simulations comprising root mean square deviation (RMSD), root mean square fluctuation (RMSF) and molecular mechanics/generalized born surface area (MM/GBSA) binding free energy calculations were carried out to check the stability of bound complexes. The drug likeness and the pharmacokinetic properties of the selected molecules were also checked through the Lipinski filter and ADMETSAR analysis. All these bioactive compounds demonstrated strong binding affinity with AChE, BACE1 and synapsin I, II and III. The results showed UA and RA to be potential inhibitors of AChE and BACE1, exhibiting binding energies comparable to those of donepezil, used as a positive control. The drug likeness and pharmacokinetic properties of these compounds also demonstrated drug-like characteristics, indicating the need for further in vitro and in vivo investigations to ascertain their therapeutic potential for AD.
  20. Fulltext TARS: A Novel Mechanism for Truly Autonomous Resource Selection in LTE-V2V Mode 4
    Khan IA, Shah SAA, Akhunzada A, Gani A, Rodrigues JJPC
    Sensors (Basel), 2021 Nov 09;21(22).
    PMID: 34833507 DOI: 10.3390/s21227431
    Effective communication in vehicular networks depends on the scheduling of wireless channel resources. There are two types of channel resource scheduling in Release 14 of the 3GPP, i.e., (1) controlled by eNodeB and (2) a distributed scheduling carried out by every vehicle, known as Autonomous Resource Selection (ARS). The most suitable resource scheduling for vehicle safety applications is the ARS mechanism. ARS includes (a) counter selection (i.e., specifying the number of subsequent transmissions) and (b) resource reselection (specifying the reuse of the same resource after counter expiry). ARS is a decentralized approach for resource selection. Therefore, resource collisions can occur during the initial selection, where multiple vehicles might select the same resource, hence resulting in packet loss. ARS is not adaptive towards vehicle density and employs a uniform random selection probability approach for counter selection and reselection. As a result, it can prevent some vehicles from transmitting in a congested vehicular network. To this end, the paper presents Truly Autonomous Resource Selection (TARS) for vehicular networks. TARS considers resource allocation as a problem of locally detecting the selected resources at neighbor vehicles to avoid resource collisions. The paper also models the behavior of counter selection and resource block reselection on resource collisions using the Discrete Time Markov Chain (DTMC). Observation of the model is used to propose a fair policy of counter selection and resource reselection in ARS. The simulation of the proposed TARS mechanism showed better performance in terms of resource collision probability and the packet delivery ratio when compared with the LTE Mode 4 standard and with a competing approach proposed by Jianhua He et al.
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