Displaying publications 61 - 80 of 159 in total

Abstract:
Sort:
  1. Dietary sodium intake and its association with hypertension: A cross-sectional study in Selangor, Malaysia
    Isa ZM, Ibrahim N, Ismail NH, Jaafar MH, Tamil AM, Yusof KH
    J Pak Med Assoc, 2021 Feb;71(Suppl 2)(2):S68-S73.
    PMID: 33785945
    OBJECTIVE: To identify the prevalence of hypertension and its relationship with dietary sodium intake among the Malay population in Selangor, Malaysia.

    Methods: Respondents were recruited from the year 2013 to 2015 from households in Klang Valley (urban area) and several settlements of the Federal Land Development Authority (FELDA) in Selangor (rural area). Data were collected using two questionnaires, a sociodemographic questionnaire and a food frequency questionnaire.

    RESULTS: A total of 3,453 adults participated in this study. The mean age of the respondents was 50.9 (±10.23) years. The prevalence of hypertension was 23.3%. Mean dietary sodium consumption was 3.6 (±6.63) grams/day, 1.6 grams higher than the current WHO recommendation. The prevalence of hypertension was higher among males aged 60 years and older; among rural population with low education level; among housewives and those with high dietary sodium intake. After adjusting for age, gender and marital status in a multiple logistic regression analysis, rural location (OR = 5.81) and high sodium intake (OR = 2.33) have been shown to affect the incidence of hypertension.

    CONCLUSIONS: A substantial proportion of Malay population in Selangor was hypertensive with a higher sodium intake than the WHO recommendation. Hypertension was associated with rural location and high sodium intake. Sustainable and cost-effective population-based health promotion and prevention interventions using a multi-sectoral approach are needed to ensure sufficient community sodium intake.

  2. Fulltext New Experimental Zirconia-Reinforced Rice Husk Nanohybrid Composite and the Outcome of Its Surface Roughness and Microhardness in Comparison with Commercialized Nanofilled and Microhybrid Composite Resins
    Lin GSS, Ghani NRNA, Ismail NH, Singbal K, Noorani TY, Mamat N
    Contemp Clin Dent, 2021 03 20;12(1):21-27.
    PMID: 33967533 DOI: 10.4103/ccd.ccd_298_20
    Background: An ideal composite resin should demonstrate smooth surface after polishing and high hardness value to provide long-term success. Thus, this study aimed to compare the surface roughness and microhardness of new experimental zirconia-reinforced rice husk nanohybrid composite (Zr-Hybrid) with commercialized nanofilled (Filtek-Z350-XT) and microhybrid composite (Zmack-Comp) resins before and after artificial ageing.

    Methods: One hundred and eighty standardized disc samples were prepared, of which ninety samples each were used for surface roughness and microhardness test, respectively. They were divided equally into: Group 1 (Filtek-Z350-XT), Group 2 (Zmack-Comp), and Group 3 (Zr-Hybrid). For surface roughness test, all samples were polished with aluminium oxide discs and further subdivided into aged and unaged subgroups, in which composite samples in aged subgroups were subjected to 2500 thermal cycles. Next, all the samples were subjected to surface roughness test using a contact stylus profilometer. As for microhardness test, all the aged and unaged samples were tested using a Vickers hardness machine with a load of 300 kgf for 10 s and viewed under a digital microscope to obtain microhardness value. Data were analyzed using two-way ANOVA followed by post hoc Tukey's honestly significant difference and paired sample t-test with significance level set at P = 0.05.

    Results: In both the aged and unaged groups, Zr-Hybrid showed statistically significantly lower surface roughness (P < 0.05) than Filtek-Z350-XT and Zmack-Comp, but no statistically significant difference was noted between Filtek-Z350-XT and Zmack-Comp (P > 0.05). A similar pattern was noted in microhardness test, whereby Zr-Hybrid showed the highest value (P < 0.05) followed by Filtek-Z350-XT and lastly Zmack-Comp. Besides, significant differences in surface roughness and microhardness were noted between the aged and unaged groups.

    Conclusion: Zr-Hybrid seems to demonstrate better surface roughness and microhardness value before and after artificial ageing.

  3. Fulltext The Physicochemical Characteristics of Gelam Honey and Its Outcome on the Female Reproductive Tissue of Sprague-Dawley Rats: A Preliminary Study
    Ismail NH, Osman K, Zulkefli AF, Mokhtar MH, Ibrahim SF
    Molecules, 2021 Jun 02;26(11).
    PMID: 34199433 DOI: 10.3390/molecules26113346
    Gelam honey (GH) is a prized natural product synthesized from the nectar of flowers from Gelam trees (Melaleuca sp.). Gelam is an evergreen tree species that grows in tropical regions such as Malaysia. GH is a multifloral honey with proven antioxidant and anti-inflammatory properties. However, the beneficial effect of GH on female reproductive tissue has yet to be substantiated. Herein, we investigated the effects of GH administration on the uterine and vaginal epithelial thickness of sexually mature Sprague-Dawley rats. Epithelia thickness could be an indicator of an atrophy manifesting as a symptom of a cardio syndrome. Rats were given oral doses of GH in four groups for 14 days; the lowest dose was 0.2 g GH/kg body weight (bw) rat/day and the highest dose was 8 g GH/kg bw rat/day. The physicochemical characteristics of GH were assessed through hydroxymethylfurfural and moisture content determination and sugar identification. GH attenuated the atrophy of the uterine and vaginal epithelia and increased the thickness of the endometrial stroma and endometrial surface endothelial layer. However, the dissonance observed in the effect of GH administration on the vaginal epithelium requires further investigation. Nevertheless, GH may have a strong potential in attenuating uterine and vaginal atrophies.
  4. Synthesis of novel bisindolylmethanes: New carbonic anhydrase II inhibitors, docking, and 3D pharmacophore studies
    Imran S, Taha M, Ismail NH, Fayyaz S, Khan KM, Choudhary MI
    Bioorg Chem, 2016 10;68:90-104.
    PMID: 27474804 DOI: 10.1016/j.bioorg.2016.07.011
    In this study, 45 bisindolylmethanes having sulfonamide moiety had been synthesized through 3 steps. In vitro assay for inhibition of carbonic anhydrase showed that some of the compounds having sulfonamide moiety are capable of inhibiting carbonic anhydrase II. Bisindoles having halogens at fifth position showed better inhibitory activity as compared to unsubstituted bisindoles. The results obtained from in vitro inhibitory activity were subjected through 3D QSAR and docking studies to identify important features contributing to the activity and further improve the structure. Pharmacophore studies suggest that bisindolylmethane moiety is contributing significantly towards the inhibition activity. Docking studies showed that compounds having nitro substituent (5g and 5i) were found to be able interact with Zn(2+) ion, Thr199, His94, His96, and His119, which interferes with the ZnOHThr199Glu106 hydrogen bond network. Bulky nitro substituent at ortho position for compound 5g prevents the compound from interacting with other residues like Thr199 and Thr200. Methyl substituent at ortho position for Compound 5i induces less steric hindrance effect, thus allowing second oxygen atom of sulfonamide to interact with Thr199 (2.51Å). Hydrogen bonding between NH on indole ring with Glu69 might have increased stability of ligand-receptor complex.
  5. Syntheses of new 3-thiazolyl coumarin derivatives, in vitro α-glucosidase inhibitory activity, and molecular modeling studies
    Salar U, Taha M, Khan KM, Ismail NH, Imran S, Perveen S, et al.
    Eur J Med Chem, 2016 Oct 21;122:196-204.
    PMID: 27371923 DOI: 10.1016/j.ejmech.2016.06.037
    3-Thiazolylcoumarin derivatives 1-14 were synthesized via one-pot two step reactions, and screened for in vitro α-glucosidase inhibitory activity. All compounds showed inhibitory activity in the range of IC50 = 0.12 ± 0.01-16.20 ± 0.23 μM as compared to standard acarbose (IC50 = 38.25 ± 0.12 μM), and also found to be nontoxic. Molecular docking study was carried out in order to establish the structure-activity relationship (SAR) which demonstrated that electron rich centers at one and electron withdrawing centers at the other end of the molecules showed strong inhibitory activity. All the synthesized compounds were characterized by spectroscopic techniques such as EI-MS, HREI-MS, (1)H NMR and (13)C NMR. CHN analysis was also performed.
  6. Molecular hybridization conceded exceptionally potent quinolinyl-oxadiazole hybrids through phenyl linked thiosemicarbazide antileishmanial scaffolds: In silico validation and SAR studies
    Taha M, Ismail NH, Ali M, Rashid U, Imran S, Uddin N, et al.
    Bioorg Chem, 2017 04;71:192-200.
    PMID: 28228228 DOI: 10.1016/j.bioorg.2017.02.005
    The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover a novel series of compounds 6-23 based on the concept of molecular hybridization. Most of the synthesized analogues exhibited potent leishmanicidal potential. The most potent compound (23, IC50=0.10±0.001μM) among the series was found ∼70 times more lethal than the standard drug. The current series 6-23 conceded in the development of fourteen (14) extraordinarily active compounds against leishmaniasis. In silico analysis were also performed to probe the mode of action while all the compounds structure were established by NMR and Mass spectral analysis.
  7. Biology-oriented drug synthesis (BIODS): In vitro β-glucuronidase inhibitory and in silico studies on 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl aryl carboxylate derivatives
    Salar U, Khan KM, Taha M, Ismail NH, Ali B, Qurat-Ul-Ain, et al.
    Eur J Med Chem, 2017 Jan 05;125:1289-1299.
    PMID: 27886546 DOI: 10.1016/j.ejmech.2016.11.031
    Current study is based on the biology-oriented drug synthesis (BIODS) of 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl aryl carboxylate derivatives 1-26, by treating metronidazole with different aryl and hetero-aryl carboxylic acids in the presence of 1,1'-carbonyl diimidazole (CDI) as a coupling agent. Structures of all synthetic derivatives were confirmed with the help of various spectroscopic techniques such as EI-MS, (1)H -NMR and (13)C NMR. CHN elemental analyses were also found in agreement with the calculated values. Synthetic derivatives were evaluated to check their β-glucuronidase inhibitory activity which revealed that except few derivatives, all demonstrated good inhibition in the range of IC50 = 1.20 ± 0.01-60.30 ± 1.40 μM as compared to the standard d-saccharic acid 1,4-lactone (IC50 = 48.38 ± 1.05 μM). Compounds 1, 3, 4, 6, 9-19, and 21-24 were found to be potent analogs and showed superior activity than standard. Limited structure-activity relationship is suggested that the molecules having electron withdrawing groups like NO2, F, Cl, and Br, were displayed better activity than the compounds with electron donating groups such as Me, OMe and BuO. To verify these interpretations, in silico study was also performed, a good correlation was observed between bioactivities and docking studies.
  8. Synthesis and biological evaluation of indole derivatives as α-amylase inhibitor
    Imran S, Taha M, Selvaraj M, Ismail NH, Chigurupati S, Mohammad JI
    Bioorg Chem, 2017 08;73:121-127.
    PMID: 28648924 DOI: 10.1016/j.bioorg.2017.06.007
    A series of twenty indole hydrazone analogs (1-21) were synthesized, characterized by different spectroscopic techniques such as 1H NMR and EI-MS, and screened for α-amylase inhibitory activity. All analogs showed a variable degree of α-amylase inhibition with IC50 values ranging between 1.66 and 2.65μM. Nine compounds that are 1 (2.23±0.01μM), 8 (2.44±0.12μM), 10 (1.92±0.12μM), 12 (2.49±0.17μM), 13 (1.66±0.09μM), 17 (2.25±0.1μM), 18 (1.87±0.25μM), 20 (1.83±0.63μM), and 19 (1.97±0.02μM) showed potent α-amylase inhibition when compared with the standard acarbose (1.05±0.29μM). Other analogs showed good to moderate α-amylase inhibition. The structure activity relationship is mainly focusing on difference of substituents on phenyl part. Molecular docking studies were carried out to understand the binding interaction of the most active compounds.
  9. Synthesis of indole analogs as potent β-glucuronidase inhibitors
    Baharudin MS, Taha M, Imran S, Ismail NH, Rahim F, Javid MT, et al.
    Bioorg Chem, 2017 06;72:323-332.
    PMID: 28505547 DOI: 10.1016/j.bioorg.2017.05.005
    Natural products are the main source of motivation to design and synthesize new molecules for drug development. Designing new molecules against β-glucuronidase inhibitory is utmost essential. In this study indole analogs (1-35) were synthesized, characterized using various spectroscopic techniques including 1H NMR and EI-MS and evaluated for their β-glucuronidase inhibitory activity. Most compounds were identified as potent inhibitors for the enzyme with IC50 values ranging between 0.50 and 53.40μM, with reference to standard d-saccharic acid 1,4-lactone (IC50=48.4±1.25μM). Structure-activity relationship had been also established. The results obtained from docking studies for the most active compound 10 showed that hydrogen bond donor features as well as hydrogen bonding with (Oε1) of nucleophilic residue Glu540 is believed to be the most importance interaction in the inhibition activity. It was also observed that hydroxyl at fourth position of benzylidene ring acts as a hydrogen bond donor and interacts with hydroxyl (OH) on the side chain of catalysis residue Tyr508. The enzyme-ligand complexed were being stabilized through electrostatic π-anion interaction with acid-base catalyst Glu451 (3.96Å) and thus preventing Glu451 from functioning as proton donor residue.
  10. Synthesis and in silico studies of novel sulfonamides having oxadiazole ring: As β-glucuronidase inhibitors
    Taha M, Baharudin MS, Ismail NH, Selvaraj M, Salar U, Alkadi KA, et al.
    Bioorg Chem, 2017 04;71:86-96.
    PMID: 28160943 DOI: 10.1016/j.bioorg.2017.01.015
    Novel sulfonamides having oxadiazole ring were synthesized by multistep reaction and evaluated to check in vitro β-glucuronidase inhibitory activity. Luckily, except compound 13, all compounds were found to demonstrate good inhibitory activity in the range of IC50=2.40±0.01-58.06±1.60μM when compared to the standard d-saccharic acid 1,4-lactone (IC50=48.4±1.25μM). Structure activity relationship was also presented. However, in order to ensure the SAR as well as the molecular interactions of compounds with the active site of enzyme, molecular docking studies on most active compounds 19, 16, 4 and 6 was carried out. All derivatives were fully characterized by 1H NMR, 13C NMR and EI-MS spectroscopic techniques. CHN analysis was also presented.
  11. Synthesis, molecular docking studies of hybrid benzimidazole as α-glucosidase inhibitor
    Zawawi NK, Taha M, Ahmat N, Ismail NH, Wadood A, Rahim F
    Bioorg Chem, 2017 02;70:184-191.
    PMID: 28043716 DOI: 10.1016/j.bioorg.2016.12.009
    Thiourea derivatives having benzimidazole 1-17 have been synthesized, characterized by 1H NMR, 13C NMR and EI-MS and evaluated for α-glucosidase inhibition. Identification of potential α-glucosidase inhibitors were done by in vitro screening of 17 thiourea bearing benzimidazole derivatives using Baker's yeast α-glucosidase enzyme. Compounds 1-17 exhibited a varying degree of α-glucosidase inhibitory activity with IC50 values between 35.83±0.66 and 297.99±1.20μM which are more better than the standard acarbose (IC50=774.5±1.94μM). Compound 10 and 14 showed significant inhibitory effects with IC50 value 50.57±0.81 and 35.83±0.66μM, respectively better than the rest of the series. Structure activity relationships were established. Molecular docking studies were performed to understand the binding interaction of the compounds.
  12. Differentiation of Ficus deltoidea varieties and chemical marker determination by UHPLC-TOFMS metabolomics for establishing quality control criteria of this popular Malaysian medicinal herb
    Afzan A, Kasim N, Ismail NH, Azmi N, Ali AM, Mat N, et al.
    Metabolomics, 2019 Mar 04;15(3):35.
    PMID: 30830457 DOI: 10.1007/s11306-019-1489-2
    BACKGROUND: Ficus deltoidea Jack (Moraceae) is a plant used in Malaysia for various diseases including as a supplement in diabetes management. Morphology distinction of the 7 main varieties (var. angustifolia, var. bilobata, var. deltoidea, var. intermedia, var. kunstleri, var. motleyana and var. trengganuensis) is challenging due to the extreme leaf heterophylly and unclear varietal boundaries, making it difficult for quality control of F. deltoidea products.

    OBJECTIVE: We aimed to compare the phytochemical composition of 7 varieties growing in different conditions at various geographical locations. We also aimed to establish the quality control markers for the authentication of these varieties.

    METHODS: We applied untargeted UHPLC-TOFMS metabolomics to discriminate 100 leaf samples of F. deltoidea collected from 6 locations in Malaysia. A genetic analysis on 21 leaf samples was also performed to validate the chemotaxonomy differentiation.

    RESULTS: The PCA and HCA analysis revealed the existence of 3 chemotypes based on the differentiation in the flavonoid content. The PLS-DA analysis identified 15 glycosylated flavone markers together with 1 furanocoumarin. These markers were always consistent for the respective varieties, regardless of the geographical locations and growing conditions. The chemotaxonomy differentiation was in agreement with the DNA sequencing. In particular, var. bilobata accession which showed divergent morphology was also differentiated by the chemical fingerprints and genotype.

    CONCLUSION: Chemotype differentiation based on the flavonoid fingerprints along with the proposed markers provide a powerful identification tool to complement morphology and genetic analyses for the quality control of raw materials and products from F. deltoidea.

  13. Fulltext Screening of medicinal plants from Taman Herba Perlis for Acetylcholinesterase inhibitory activity
    Abdul Somat N, Osman CP, Ismail NH, Yusoff Z, Md Yusof Y
    Science Letters, 2019;13(1):23-32.
    MyJurnal
    In a search for new potential AChE inhibitors, 31 selected medicinal plants from Perlis were collected gathered, air dried and successively extracted using hexane, dichloromethane, and alcohol. The dichloromethane and alcoholic extracts were screened for AChE inhibitory activity using Ellman's method. Out of 31 plant species, the methanol extracts of Rhapis excelsa leaves (97.03 ± 3.71 %), Diospyros blancoi leaves (95.80 ± 1.57 %) and Phyllantus elegans root (83.22 ± 3.08 %) showed the highest AChE inhibitory activity at the concentration of 100 μg/mL.
  14. Novel dental composite resin derived from rice husk natural biowaste: A systematic review and recommendation for future advancement
    Lin GSS, Cher CY, Cheah KK, Noorani TY, Ismail NH, Ghani NRNA
    J Esthet Restor Dent, 2021 Oct 30.
    PMID: 34716755 DOI: 10.1111/jerd.12831
    OBJECTIVES: This review aimed to summarize contemporary evidence related to dental composite resin derived from rice husk biowaste and its potential future advancement. This review paper included the techniques for synthesis, characterization, and preparation of rice husk composite resin. Focus was also given to the flexural strength and modulus, compressive strength, wear rate, hardness, surface roughness, color stability, polymerization shrinkage, degree of conversion, and their application onto root canal treated teeth.

    MATERIAL AND METHODS: A search of English peer-reviewed literature (January 1960-February 2021) was conducted from electronic databases (PubMed Central, Cochrane, LILACS, Science Direct, Web of Science, SIGLE, EMBASE, EBSCO, Medline, and Google Scholar).

    RESULTS: 11 articles and a book section were finally selected for qualitative analysis. Studies concluded that the physicomechanical properties and the color stability of rice husk dental composites showed comparable results to conventional dental composites. Incorporation of zirconia nanopowder into rice husk dental composite increased the compressive strength and hardness values, associated with lower shrinkage, a high degree of conversion, and improved fracture strength when applied on root canal treated teeth.

    CONCLUSIONS: Due to its low cost, eco-friendliness, and acceptable clinical performances, rice husk dental composite resin can be considered as an alternative to conventional composites.

    CLINICAL SIGNIFICANCE: Dental composite resin derived from rice husk silica demonstrated excellent performance, which could potentially substitute currently available composite resins. This review will give new insight to clinicians and researchers on the usage of natural biowaste mass in the field of dental restorative materials.

  15. Synthesis, β-glucuronidase inhibition and molecular docking studies of cyano-substituted bisindole hydrazone hybrids
    Abid O, Imran S, Taha M, Ismail NH, Jamil W, Kashif SM, et al.
    Mol Divers, 2021 May;25(2):995-1009.
    PMID: 32301032 DOI: 10.1007/s11030-020-10084-4
    The β-glucuronidase, a lysosomal enzyme, catalyzes the cleavage of glucuronosyl-O-bonds. Its inhibitors play a significant role in different medicinal therapies as they cause a decrease in carcinogen-induced colonic tumors by reducing the level of toxic substances present in the intestine. Among those inhibitors, bisindole derivatives had displayed promising β-glucuronidase inhibition activity. In the current study, hydrazone derivatives of bisindolymethane (1-30) were synthesized and evaluated for in vitro β-glucuronidase inhibitory activity. Twenty-eight analogs demonstrated better activity (IC50 = 0.50-46.5 µM) than standard D-saccharic acid 1,4-lactone (IC50 = 48.4 ± 1.25 µM). Compounds with hydroxyl group like 6 (0.60 ± 0.01 µM), 20 (1.50 ± 0.10 µM) and 25 (0.50 ± 0.01 µM) exhibited the most potent inhibitory activity, followed by analogs with fluorine 21 (3.50 ± 0.10 µM) and chlorine 23 (8.20 ± 0.20 µM) substituents. The presence of hydroxyl group at the aromatic side chain was observed as the main contributing factor in the inhibitory potential. From the docking studies, it was predicted that the active compounds can fit properly in the binding groove of the β-glucuronidase and displayed significant binding interactions with essential residues.
  16. Synthesis, in vitro β-glucuronidase inhibitory potential and molecular docking studies of quinolines
    Bano B, Arshia, Khan KM, Kanwal, Fatima B, Taha M, et al.
    Eur J Med Chem, 2017 Oct 20;139:849-864.
    PMID: 28865280 DOI: 10.1016/j.ejmech.2017.08.052
    In this study synthesis and β-glucuronidase inhibitory potential of 3/5/8 sulfonamide and 8-sulfonate derivatives of quinoline (1-40) are discussed. Studies reveal that all the synthetic compounds were found to have good inhibitory activity against β-glucuronidase. Nonetheless, compounds 1, 2, 5, 13, and 22-24 having IC50 values in the range of 1.60-8.40 μM showed superior activity than the standard saccharic acid 1,4-lactone (IC50 = 48.4 ± 1.25 μM). Moreover, molecular docking studies of selected compounds were also performed to see interactions between active compounds and binding sites. Structures of all the synthetic compounds were confirmed through (1)H NMR, EI-MS and HREI-MS spectroscopic techniques.
  17. Fulltext Assessing the nutritional status of hospitalized elderly
    Abd Aziz NAS, Teng NIMF, Abdul Hamid MR, Ismail NH
    Clin Interv Aging, 2017;12:1615-1625.
    PMID: 29042762 DOI: 10.2147/CIA.S140859
    PURPOSE: The increasing number of elderly people worldwide throughout the years is concerning due to the health problems often faced by this population. This review aims to summarize the nutritional status among hospitalized elderly and the role of the nutritional assessment tools in this issue.

    METHODS: A literature search was performed on six databases using the terms "malnutrition", "hospitalised elderly", "nutritional assessment", "Mini Nutritional Assessment (MNA)", "Geriatric Nutrition Risk Index (GNRI)", and "Subjective Global Assessment (SGA)".

    RESULTS: According to the previous studies, the prevalence of malnutrition among hospitalized elderly shows an increasing trend not only locally but also across the world. Under-recognition of malnutrition causes the number of malnourished hospitalized elderly to remain high throughout the years. Thus, the development of nutritional screening and assessment tools has been widely studied, and these tools are readily available nowadays. SGA, MNA, and GNRI are the nutritional assessment tools developed specifically for the elderly and are well validated in most countries. However, to date, there is no single tool that can be considered as the universal gold standard for the diagnosis of nutritional status in hospitalized patients.

    CONCLUSION: It is important to identify which nutritional assessment tool is suitable to be used in this group to ensure that a structured assessment and documentation of nutritional status can be established. An early and accurate identification of the appropriate treatment of malnutrition can be done as soon as possible, and thus, the malnutrition rate among this group can be minimized in the future.

  18. Synthesis of piperazine sulfonamide analogs as diabetic-II inhibitors and their molecular docking study
    Taha M, Irshad M, Imran S, Chigurupati S, Selvaraj M, Rahim F, et al.
    Eur J Med Chem, 2017 Dec 01;141:530-537.
    PMID: 29102178 DOI: 10.1016/j.ejmech.2017.10.028
    Piperazine Sulfonamide analogs (1-19) have been synthesized, characterized by different spectroscopic techniques and evaluated for α-amylase Inhibition. Analogs 1-19 exhibited a varying degree of α-amylase inhibitory activity with IC50 values ranging in between 1.571 ± 0.05 to 3.98 ± 0.397 μM when compared with the standard acarbose (IC50 = 1.353 ± 0.232 μM). Compound 1, 2, 3 and 7 showed significant inhibitory effects with IC50 value 2.348 ± 0.444, 2.064 ± 0.04, 1.571 ± 0.05 and 2.118 ± 0.204 μM, respectively better than the rest of the series. Structure activity relationships were established. Molecular docking studies were performed to understand the binding interaction of the compounds.
  19. Hydrazinyl arylthiazole based pyridine scaffolds: Synthesis, structural characterization, in vitro α-glucosidase inhibitory activity, and in silico studies
    Ali F, Khan KM, Salar U, Taha M, Ismail NH, Wadood A, et al.
    Eur J Med Chem, 2017 Sep 29;138:255-272.
    PMID: 28672278 DOI: 10.1016/j.ejmech.2017.06.041
    Acarbose, miglitol, and voglibose are the inhibitors of α-glucosidase enzyme and being clinically used for the management of type-II diabetes mellitus. However, many adverse effects are also associated with them. So, the development of new therapeutic agents is an utmost interest in medicinal chemistry research. Current study is based on the identification of new α-glucosidase inhibitors. For that purpose, hydrazinyl arylthiazole based pyridine derivatives 1-39 were synthesized via two step reaction and fully characterized by spectroscopic techniques EI-MS, HREI-MS, (1)H-, and (13)C NMR. However, stereochemistry of the iminic bond was confirmed by NOESY. All compounds were subjected to in vitro α-glucosidase inhibitory activity and found many folds active (IC50 = 1.40 ± 0.01-236.10 ± 2.20 μM) as compared to the standard acarbose having IC50 value of 856.45 ± 5.60 μM. A limited structure-activity relationship was carried out in order to make a presumption about the substituent's effect on inhibitory activity which predicted that substituents of more negative inductive effect played important role in the activity as compared to the substituents of less negative inductive effect. However, in order to have a good understanding of ligand enzyme interactions, molecular docking study was also conducted. In silico study was confirmed that substituents like halogens (Cl) and nitro (NO2) which have negative inductive effect were found to make important interactions with active site residues.
  20. Sociotechnical factors influencing unsafe use of hospital information systems: A qualitative study in Malaysian government hospitals
    Salahuddin L, Ismail Z, Hashim UR, Raja Ikram RR, Ismail NH, Naim Mohayat MH
    Health Informatics J, 2019 12;25(4):1358-1372.
    PMID: 29521162 DOI: 10.1177/1460458218759698
    The objective of this study is to identify factors influencing unsafe use of hospital information systems in Malaysian government hospitals. Semi-structured interviews with 31 medical doctors in three Malaysian government hospitals implementing total hospital information systems were conducted between March and May 2015. A thematic qualitative analysis was performed on the resultant data to deduce the relevant themes. A total of five themes emerged as the factors influencing unsafe use of a hospital information system: (1) knowledge, (2) system quality, (3) task stressor, (4) organization resources, and (5) teamwork. These qualitative findings highlight that factors influencing unsafe use of a hospital information system originate from multidimensional sociotechnical aspects. Unsafe use of a hospital information system could possibly lead to the incidence of errors and thus raises safety risks to the patients. Hence, multiple interventions (e.g. technology systems and teamwork) are required in shaping high-quality hospital information system use.
Related Terms
Filters
Contact Us

Please provide feedback to Administrator (afdal@afpm.org.my)

External Links