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  1. Zuraida, A., Maisarah, T., Zahurin, H., Muhammad Luqman, A., Roszaliya, A., Wan Shazlin Maisarah, W.M.Y., et al.
    MyJurnal
    The chemical composition and anatomical characteristics on lignin distribution of rattan waste were analyzed to determine its suitability to be used in binderless board fabrication. The chemical composition was analyzed by using TAPPI methods. Observation and determination of lignin distribution and board structure were executed by using optical microscopy (OM) and scanning electron microscope (SEM). High amount of hemicellulose, cellulose and lignin content found in rattan waste chemical composition is seen to help in binderless board fabrication. The micrographs revealed that the rattan has fine structural construction that helps in producing good qualities of binderless boards with particular manufacturing parameters.
  2. Wan Ismahanisa Ismail, Mohamed Azmi Ahmad Hassali, Farooqui, Maryam, Saleem Fahad, Wan Rohani Wan Taib, Muhammad Nabil Fikri Roslan
    MyJurnal
    HRQOL is referring to patients' perceptions that is related to physical and mental of thalessemia patients. HRQOL measurement is crucial in assessing the extent of impact that this chronic disease has affected the thalassaemia patients’ lives. HRQOL measurement also includes identifying the effects of the treatment and disease towards wellbeing of the patients. Quality of Life (QOL) of individuals with thalassaemia major are affected by many influence factors such as the effect of diagnosis and treatment, chronic conditions state, appearances, treatment’s components such as frequent hospital visits for the transfusion, nightly mixture of subcutaneous, late arrival or absence, sexual development and complications from the disease[1-2].

    The study aims to assess the Health Related Quality of Life (HRQoL) among thalassaemia patients and identify the significant factors that contribute to HRQoL in thalassaemia patients in Malaysia. A cross sectional based study was conducted at Kedah Thalassaemia Society Club in Kedah, Malaysia. The HRQoL was measured using a Short form survey version 2 (SF-36). Descriptive study was used to describe the demographic and disease related to the thalassaemia patients. The HRQoL was compared using the Mann-Whitney and Kruskal-Wallis test. The analyses were performed using the Quality Metric Health Outcomes Scoring software for SF-36 and SPSS v 22. Three hundred and ninety thalassaemia patients were enrolled in the study. The majority of the participants (n = 221, 58.5%) were categorized in the age group of 18-27 years (25.40 ± 10.2). The HRQoL measure of less than 50 for the physical component summary (PCS) and mental component summary (MCS) among thalassaemia patients were rated as poor. Patients with higher education levels were significantly associated with PCS (p=0.002) and showed higher mean scores for PCS (52.0) compared to the others. Age, marital status, employment status, monthly income, health check-ups before screening of thalassaemia and medical insurance was associated with PCS levels compare to the others. The type of thalassaemia, the medical treatment received and the side effects of the conventional treatment were significantly associated with p-values of less than 0.001 and PCS and MCS scores of below 50.
  3. Goh, E.H., Tan, G.H., Rozman, Z., Nik Azuan, N.I., Fam, X.I., Mohd Hafidzul, J., et al.
    MyJurnal
    Hematospermia is a distressing disorder in sexually active men resulting in great concern to the patient. We report an unusual case of hematospermia with an atypical presentation, involving a 54-year-old man presented with acute urinary retention after sexual intercourse. Although the causes are widely known, arteriovenous malformation as the cause of this disorder has not much been reported in the literature. Transcatheter embolization of internal pudendal artery is a promising option for hematospermia caused by arterial fistula or bleeding.
  4. Muhammad Faiz Mohd Ismail, smarulyusda Isha, Syarif Husin Lubis, Nur Zakiah Mohd Saat, Siti Nor Ismalina Isa, Normah Che Din
    Jurnal Sains Kesihatan Malaysia, 2017;15(1):105-112.
    MyJurnal
    This paper investigate the effect of parents’ education background and family monthly income on the Intelligence Quotient
    (IQ) of students with special needs in Kelantan, Malaysia. This cross-sectional method study was employed multistage
    random sampling to obtain information drawn from 130 participants from 10 selected school in Kelantan, Malaysia.
    Questionnaire was used to obtain parents’ education background, family monthly income and demographic variables.
    Students IQ were assessed using Comprehensive Test for Non-Verbal Intelligence (CTONI 2nd Edition). Data analysis involve
    independent sample t-test, one-way between group ANOVA, Pearson’s correlation and multiple linear regression. From
    analysis of IQ score, 63.8% of the special needs students scored very poor IQ, 12.3% scored below average and only
    1.5% score average IQ. Significant mean difference were revealed between age group (p = 0.002), parents’ education (p
    = 0.018) and family monthly income (p < 0.05) on special needs students IQ. Post-hoc tukey shows significance between
    parents who never went to school, went to secondary school (p = 0.037) and university/college (p = 0.021). In term of
    family monthly income, significance difference were found between family with low and high monthly income (p < 0.05).
    Family monthly income (r = 0.393, p < 0.01) showed positive moderate correlation on special needs students IQ. After
    being forwarded by multiple linear regression, it was found that family monthly income (B = 3.605, p < 0.05) and age
    group of special needs students (B = 0.879, p = 0.002) were significant predictor for IQ score and explained 22.5% of
    the variance (R2
    = 0.225, F (5,124) = 83.94, p < 0.05. Overally, majority of special needs students in current study have
    very poor IQ score. Further explanation are discussed on the paper.
  5. Norafiza Zainuddin, Lailatul Jalilah Mohd Ridah, Aqilah Nabihah Omar, Norlelawati A. Talib, Naznin Muhammad, Faezahtul Arbaeyah Hussain
    MyJurnal
    MGMT (O6
    -Methylguanine-DNA Methyltransferase) suppresses tumor development by removing alkyl adduct, while
    SPOCK2 (SPARC/Osteonectin CWCV and Kazal-like domains proteoglycan) abolishes the inhibition of membrane-type
    matrix metalloproteinases (MT-MMP) which leads to angiogenesis. Hence, MGMT methylation may initiate malignant cells
    transformation. In contrast, SPOCK2 methylation is hypothesized not to be a common event in diffuse large B-cell lymphoma
    (DLBCL). In this study, we examined the methylation status of MGMT and SPOCK2 in DLBCL as in Malaysia the information
    is extremely lacking. A total of 88 formalin-fixed paraffin-embedded tissue of patients diagnosed with DLBCL from the
    year 2006 to 2013 were retrieved from Hospital Universiti Sains Malaysia, Kelantan and Hospital Tengku Ampuan Afzan,
    Pahang. Methylation-specific polymerase chain reaction (MSP) was used to examine the methylation status of both genes.
    Interestingly, methylation of MGMT was detected in all the 88 DLBCL samples, whereas SPOCK2 was found to be methylated
    in 83 of 88 (94.3%) DLBCL cases. Our study showed a remarkably high percentage of promoter methylation of both
    MGMT and SPOCK2 genes. Our finding also negates initial expectation that SPOCK2 methylation would be an uncommon
    event in the majority of DLBCL cases. This study has shown a very high percentage of promoter methylation of MGMT and
    SPOCK2 in the DLBCL cases studied by MSP, using archival lymphoma tissues. Nonetheless, additional research is needed
    to quantitatively evaluate MGMT and SPOCK2 methylation, and to analyse gene expression and/or protein expression in
    order to further understand the role of MGMT and SPOCK2 methylation in the pathogenesis of DLBCL.
  6. Hamid Ali Nagi Al-Jamal, Wan Rohani Wan Taib, Siti Asmaa Mat Jusoh, Aziee Sudin, Muhammad Farid Johan
    MyJurnal
    Azacytidine (5-Aza) is a chemotherapeutic drug that has been known to restore the expression of Tumour suppressor genes by de-methylation and shown clinical efficacy inMyelodysplastic syndrome (MDS) [1-3]. Currently, 5-Aza is being used in UK for the treatment of some adults with MDS, chronic myelocytic leukemia (CML) and acute myelocytic leukemia (AML) [4]. Majority of CML patients treated with imatinib, a BCR/ABL inhibitor would develop resistance under prolonged therapy. Signal transducer and activator of transcription 3 (STAT3) is an oncogenic transcription factor that is constitutively activated in various human cancers including hematological malignancies. Activation of STAT3 represents an important mechanism of imatinib resistant [5]. Methylation of SHP-1is involved in the constitutive activation of STAT3 [6], and a low level of SHP-1is not sufficient to inhibit activated STAT3 [7]. Epigenetic silencing of SHP-1also plays a role in the development of resistance to imatinib in BCR/ABL positive CML cells.
  7. Ngah, N.A., Siti Jusna Muhammad, Suraini, M.S., Mohd Noh, M.S.F., Ab Hamid, S., Salleh, H., et al.
    MyJurnal
    Internal obstruction of the upper airways can be due to infection, anaphylactic reaction, congenital anomaly, foreign body inhalation or mass. This case report is of a lady who presented with upper airway obstruction due to subglottic ectopic thyroid tissue. She had a history of noisy breathing and progressive neck swelling since childhood. Biochemical results showed hypothyroid features while flexible scope showed tracheal stenosis. Computed Tomography (CT) detected a goitre and a posterior laryngeal mass at subglottic region causing laryngeal stenosis. The MRI helped to better delineate the soft tissue details of this mass. while elective direct laryngoscope showed a firm mass arising from the trachea. Debulking of the mass was done and histopathological diagnosis was nodular thyroid hyperplasia. Treatment with L-thyroxine was instituted with good clinical improvement. An ectopic thyroid gland can develop if its normal migration is halted along this tract during embryogenesis. Subglottic location of ectopic thyroid is extremely rare. However, ectopic thyroid tissue in the larynx should be considered as a possible diagnosis causing upper airway obstruction, especially in a patient that is clinically hypothyroid and having a concurrent goitre.
  8. Wan Nordiana W Abd Rahman, Raizulnasuha Ab Rashid, Mahfuzah Muhammad, Khairunisak Abdul Razak, Norhayati Dollah, Moshi Geso
    MyJurnal
    Gold nanoparticles (AuNPs) have been extensively investigated as dose enhancement agent to increase the lethal dose to the tumours while minimizing dose to the normal tissue. Their intriguing properties and characteristics such as small size and shape provide favorable option in increasing radiotherapy therapeutic efficiency. In this study, the effects of AuNPs size on the dose enhancement effects irradiated under megavoltage photon beams were investigated. The study was conducted in-vitro on HeLa cells using AuNPs of 5 nm and 15 nm sizes. The cells samples were incubated with AuNPs and irradiated with photon beam of energy 6 MV and 10 MV at 100 cm SSD and 10 cm x 10 cm field size. Clonogenic assay were performed to observe the dose enhancement effects on cell survival. Dose enhancement factor (DEF) were extrapolated and evaluated from the cell survival curves. The results show that both sizes of AuNPs produce dose enhancement with the larger size AuNPs of 15 nm produce more dose enhancement compare to 5 nm AuNPs for 6 MV photon beam. Dose enhancements were observed for 10 MV photon beams but DEF for both sizes AuNPs shows no differences. In conclusion, larger size AuNPs produce higher dose enhancement compare to small size of AuNPs which conclude that nanoparticles size is important factor that need to be taken into account for AuNPs to be applied in radiotherapy.
  9. Azlina Wati Nikmat, Nurul Azreen Hashim, Muhammad Farid Saidi, Nur Suhailah Mohd Zaki, Nur Nabihah Hasan Shukri, Nur Basyariah Abdulla
    MyJurnal
    Objective: Smart phones have become an important part of human’s life, including the healthcare population and medical students. However, pathological use of smart phones could lead to smart phones addiction. The aim of this study is to observe a pattern of usage of smart phones among the medical students and staffs in the Faculty of Medicine Universiti Teknologi MARA (UiTM) and screen for smart phone addiction among the respondents.

    Methods: A cross sectional, quasi-experimental study design involving medical students and staffs in the Faculty of Medicine Universiti Teknologi MARA (UiTM) was employed. A total of 598 respondents was approached to participate, and all consented to this study. Measurements used in the study include a self-developed questionnaire to measure pattern of smart phone usage and Smart phone addiction scale (Malay version).

    Result: We found that 65.9% of the respondents were heavy users of the smart phone (more than 3 hours daily) and majority of them were using it for social networking. More than half of the respondents (52.2%) were at risk of developing smart phone addiction based on Smart phone Addiction Scale (Malay Version).

    Conclusion: This study revealed that medical students, and the faculty staffs were heavy users of smart phones, and they were at risk to develop smart phone addiction.
  10. Ndlovu ST, Ullah N, Khan S, Ramharack P, Soliman M, de Matas M, et al.
    Drug Deliv Transl Res, 2019 Feb;9(1):284-297.
    PMID: 30387048 DOI: 10.1007/s13346-018-00596-w
    The aim of this study was to employ experimental and molecular modelling approaches to use molecular level interactions to rationalise the selection of suitable polymers for use in the production of stable domperidone (DOMP) nanocrystals with enhanced bioavailability. A low-energy antisolvent precipitation method was used for the preparation and screening of polymers for stable nanocrystals of DOMP. Ethyl cellulose was found to be very efficient in producing stable DOMP nanocrystals with particle size of 130 ± 3 nm. Moreover, the combination of hydroxypropyl methylcellulose and polyvinyl alcohol was also shown to be better in producing DOMP nanocrystals with smaller particle size (200 ± 3.5 nm). DOMP nanosuspension stored at 2-8 °C and at room temperature (25 °C) exhibited better stability compared to the samples stored at 40 °C. Crystallinity of the unprocessed and processed DOMP was monitored by differential scanning calorimetry and powder X-ray diffraction. DOMP nanocrystals gave enhanced dissolution rate compared to the unprocessed drug substance. DOMP nanocrystals at a dose of 10 mg/kg in rats showed enhanced bioavailability compared to the raw drug substance and marketed formulation. A significant increase in plasma concentration of 2.6 μg/mL with a significant decrease in time (1 h) to reach maximum plasma concentration was observed for DOMP nanocrystals compared to the raw DOMP. Molecular modelling studies provided underpinning knowledge at the molecular level of the DOMP-polymer nanocrystal interactions and substantiated the experimental studies. This included an understanding of the impact of polymers on the size of nanocrystals and their associated stability characteristics.
  11. Suriani Ismail, Huda Zainuddin, Titi Rahmawati Hamedon, Muhammad Hanafiah Juni, Nor Afiah Mohd. Zulkefli, Suhainizam bin Muhamad Saliluddin
    MyJurnal
    Background: Lack of awareness, poor knowledge and attitude regarding cancer have been identified as possible reasons accounting for the late presentation which lead to the poor survival of cancer patients in Malaysia. Method: A cross sectional study was conducted in three traditional Malay villages in Negeri Sembilan among adult males. Those who were already diagnosed with prostate cancer or Non malaysians were excluded from the study. Data was collected using self-administered questionnaires which consist of several sections namely socio-demographic, awareness about prostate cancer, sources of information, family history of prostate cancer, lifestyle associated with risk of cancer, knowledge and attitude towards prostate cancer. Data was analysed using SPSS version 22.0. Chisquare test was used to determine associations. Level of significance was set at p
  12. Yousuf S, Khan KM, Salar U, Chigurupati S, Muhammad MT, Wadood A, et al.
    Eur J Med Chem, 2018 Nov 05;159:47-58.
    PMID: 30268823 DOI: 10.1016/j.ejmech.2018.09.052
    Acarbose and voglibose are well-known α-amylase inhibitors used for the management of type-II diabetes mellitus. Unfortunately, these well-known and clinically used inhibitors are also associated with several adverse effects. Therefore, there is still need to develop the safer therapy. Despite of a broad spectrum of biological significances of pyrazolone, it is infrequently evaluated for α-amylase inhibition. Current study deals with the synthesis and biological screening of aryl and arylidene substituted pyrazolones 1-18 for their potential α-amylase inhibitory activity. Structures of synthetic derivatives 1-18 were identified by different spectroscopic techniques. All compounds 1-18 (IC50 = 1.61 ± 0.16 μM to 2.38 ± 0.09 μM) exhibited significant to moderate inhibitory potential when compared to standard acarbose (IC50 = 1.46 ± 0.26 μM). A number of derivatives including 8-12 (IC50 = 1.68 ± 0.1 μM to 1.97 ± 0.07 μM) and 14-16 (IC50 = 1.61 ± 0.16 μM to 1.93 ± 0.07 μM) were found to be significantly active. Limited SAR suggested that different substitutions on compounds do not have any significant effect on the inhibitory potential. Compounds were found to be mixed-type inhibitors revealed by kinetic studies. However, in silico study was identified a number of key features participating in the interaction with the binding site of α-amylase enzyme.
  13. Shehzad MT, Imran A, Njateng GSS, Hameed A, Islam M, Al-Rashida M, et al.
    Bioorg Chem, 2019 06;87:857-866.
    PMID: 30551808 DOI: 10.1016/j.bioorg.2018.12.006
    Aldose reductase is an important enzyme in the polyol pathway, where glucose is converted to fructose, and sorbitol is released. Aldose reductase activity increases in diabetes as the glucose levels increase, resulting in increased sorbitol production. Sorbitol, being less cell permeable tends to accumulate in tissues such as eye lenses, peripheral nerves and glomerulus that are not insulin sensitive. This excessive build-up of sorbitol is responsible for diabetes associated complications such as retinopathy and neuropathy. In continuation of our interest to design and discover potent inhibitors of aldo-keto reductases (AKRs; aldehyde reductase ALR1 or AKR1A, and aldose reductase ALR2 or AKR1B), herein we designed and investigated a series of new benzoxazinone-thiosemicarbazones (3a-r) as ALR2 and ALR1 inhibitors. Most compounds exhibited excellent inhibitory activities with IC50 values in lower micro-molar range. Compounds 3b and 3l were found to be most active ALR2 inhibitors with IC50 values of 0.52 ± 0.04 and 0.19 ± 0.03 μM, respectively, both compounds were more effective inhibitors as compared to the standard ALR2 inhibitor (sorbinil, with IC50 value of 3.14 ± 0.02 μM).
  14. Muhammad Najmi, K., Logeswary, K., Rona Asnida, N., Wan Haslina Wah, Umi Kalthum, M.N., Aida Zairani, M.Z.
    Medicine & Health, 2018;13(1):208-214.
    MyJurnal
    We report the case series of phacoemulsification-related Descemet membrane detachment (DMD) encountered at a tertiary hospital in Kuala Lumpur. Case 1 was an iatrogenic DMD which was detected intraoperatively and managed early with good outcome. Case 2 and case 3 described unusual presentation of DMD which was initially undiagnosed. This report highlights the use of anterior segment optical coherence tomography (ASOCT) in detecting and confirming the correct diagnosis for DMD. With the aid of an experienced corneal specialist, the higher threshold for suspicious occurrence of DMD was confirmed using ASOCT. Treatment was tailored accordingly, with successful clearance of corneal oedema and visual recovery. This case series highlighted the importance of proper operative documentation and high threshold for suspicion for DMD in focal corneal oedema following an otherwise uneventful cataract surgery. It is concluded that ASOCT is an excellent tool to confirm diagnosis of DMD and success of treatment.
  15. Ahmad U, Sohail M, Ahmad M, Minhas MU, Khan S, Hussain Z, et al.
    Int J Biol Macromol, 2019 May 15;129:233-245.
    PMID: 30738157 DOI: 10.1016/j.ijbiomac.2019.02.031
    Oral drug delivery is natural, most acceptable and desirable route for nearly all drugs, but many drugs like NSAIDs when delivered by this route cause gastrointestinal irritation, gastric bleeding, ulcers, and many undesirable effects which limits their usage by oral delivery. Moreover, it is almost impossible to control the release of a drug in a targeted location in body. We developed thermo-responsive chitosan-co-poly(N-isopropyl-acrylamide) injectable hydrogel as an alternative for the gastro-protective and controlled delivery of loxoprofen sodium as a model drug. A free radical polymerization technique was used to synthesize thermo-responsive hydrogel by cross-linking chitosan HCl with NIPAAM using glutaraldehyde as cross-linker. Confirmation of crosslinked hydrogel structure was done by Fourier transform infrared spectra (FTIR). The thermal stability of hydrogel was confirmed through thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC). The scanning electron microscopy (SEM) was performed to evaluate the structural morphology of cross-linked hydrogel. To evaluate the rheological behavior of hydrogel with increasing temperature, rheological study was performed. Swelling and in vitro drug release studies were carried out under various temperature and pH conditions. The swelling study revealed that maximum swelling was observed at low pH (pH 1.2) and low temperature (25 °C) compared to the high range of pH and temperature and it resulted in quick release of the drug. The high range of pH (7.4) and temperature (37 °C) however caused controlled release of the drug. The in vivo evaluation of the developed hydrogel in rabbits demonstrated the controlled release behavior of fabricated system.
  16. Butt ARS, Abbasi MA, Aziz-Ur-Rehman, Siddiqui SZ, Raza H, Hassan M, et al.
    Bioorg Chem, 2019 05;86:459-472.
    PMID: 30772647 DOI: 10.1016/j.bioorg.2019.01.036
    The present research was designed for the selective synthesis of novel bi-heterocyclic acetamides, 9a-n, and their tyrosinase inhibition to overwhelm the problem of melanogenesis. The structures of newly synthesized compounds were confirmed by spectral techniques such as 1H NMR, 13C NMR, and EI-MS along with elemental analysis. The inhibitory effects of these bi-heterocyclic acetamides (9a-n) were evaluated against tyrosinase and all these molecules were recognized as potent inhibitors relative to the standard used. The Kinetics mechanism was analyzed by Lineweaver-Burk plots which explored that compound, 9h, inhibited tyrosinase competitively by forming an enzyme-inhibitor complex. The inhibition constants Ki calculated from Dixon plots for this compound was 0.0027 µM. The computational study was coherent with the experimental records and these ligands exhibited good binding energy values (kcal/mol). The hemolytic analysis revealed their mild cytotoxicity towards red blood cell membranes and hence, these molecules can be pondered as nontoxic medicinal scaffolds for skin pigmentation and related disorders.
  17. Nor Azureen Rozekhi, Shahril Hussin, Ashraf Siddik Khan Abdul Rahim Siddiqe, Muhammad 'Arif Aizat Bashir, Hairul Nizwan Abd Majid
    MyJurnal
    It has been remarked that food irradiation is an emerging technology with many advantages to
    consumers. Among the benefits of food irradiation include the destruction of insects, fungi and bacteria
    that cause food to spoil and causes food borne illnesses in humans. However, there appears to be a
    lacking in widespread public awareness and understanding of food radiation for human consumption.
    Therefore, this study is attempting to investigate consumer awareness, attitude, trust and understanding
    toward food irradiation. A total of 237 respondents participated in the study via self-administered
    questionnaires. Findings revealed that consumers’ level of awareness towards food irradiation was
    surprisingly high. On the other hand, level of positive attitude and trust towards irradiated food were
    accepted. The findings of this study could contribute to the body of knowledge regarding the
    awareness, knowledge, attitude and trust towards food irradiation among consumers. In addition, it
    provides information and suggestions for the authorities in governing and imposing rules and
    regulations on food and beverage operators and handlers in Malaysia.
  18. Wan Azfarozza Wan Athmar, Nur Azmina Ghazali, Muhammad Saiful Adli Mohd Nasir, Anis Athirah Zuhaizar, Farahani Mohd Asli
    MyJurnal
    Social media are now acknowledged as one of the platforms for engaging e-health that contributing to serious discussion and information regarding on medical and health issues. However, there are challenges and risks associated with social media in medical and health care which is misinformation. Misinformation can spread quickly on Twitter and each retweet is exposing to wider audiences. The aim of this paper is to identify the use of @MedTweetMYHQ among its’ users sepcifically among UiTM Melaka students. The researchers used in-depth interviews to five informants based on purposive sampling. The data was analysed using thematic analysis. Four themes emerged from the analysis which are the use of @MedTweetMYHQ to receive updated useful information on health, to share information on healthy lifestyle, to debunk health myths and as a platform for health discussions.
  19. Abbasi MA, Nazir M, Ur-Rehman A, Siddiqui SZ, Hassan M, Raza H, et al.
    Arch Pharm (Weinheim), 2019 Mar;352(3):e1800278.
    PMID: 30624805 DOI: 10.1002/ardp.201800278
    Novel bi-heterocyclic benzamides were synthesized by sequentially converting 4-(1H-indol-3-yl)butanoic acid (1) into ethyl 4-(1H-indol-3-yl)butanoate (2), 4-(1H-indol-3-yl)butanohydrazide (3), and a nucleophilic 5-[3-(1H-indol-3-yl)propyl]-1,3,4-oxadiazole-2-thiol (4). In a parallel series of reactions, various electrophiles were synthesized by reacting substituted anilines (5a-k) with 4-(chloromethyl)benzoylchloride (6) to afford 4-(chloromethyl)-N-(substituted-phenyl)benzamides (7a-k). Finally, the nucleophilic substitution reaction of 4 was carried out with newly synthesized electrophiles, 7a-k, to acquire the targeted bi-heterocyclic benzamides, 8a-k. The structural confirmation of all the synthesized compounds was done by IR, 1 H NMR, 13 C NMR, EI-MS, and CHN analysis data. The inhibitory effects of these bi-heterocyclic benzamides (8a-k) were evaluated against alkaline phosphatase, and all these molecules were identified as potent inhibitors relative to the standard used. The kinetics mechanism was ascribed by evaluating the Lineweaver-Burk plots, which revealed that compound 8b inhibited alkaline phosphatase non-competitively to form an enzyme-inhibitor complex. The inhibition constant Ki calculated from Dixon plots for this compound was 1.15 μM. The computational study was in full agreement with the experimental records and these ligands exhibited good binding energy values. These molecules also exhibited mild cytotoxicity toward red blood cell membranes when analyzed through hemolysis. So, these molecules might be deliberated as nontoxic medicinal scaffolds to render normal calcification of bones and teeth.
  20. Amin F, Khan S, Shah SMH, Rahim H, Hussain Z, Sohail M, et al.
    Drug Des Devel Ther, 2018;12:3855-3866.
    PMID: 30510401 DOI: 10.2147/DDDT.S183534
    Background: The obnoxious bitter taste of orally taken antibiotics is one of the biggest problems in the treatment of children. The pediatric population cannot tolerate the bitter taste of drugs and vomit out which ultimately leads to suboptimal therapeutic value, grimace and mental stress so it is the challenging task for the formulation scientists to formulate a palatable formulation particularly to overcome address the issue.

    Purpose of study: The study aimed to mask and evaluate the unpleasant bitter taste of azithro-mycin (AZ) in the dry suspension dosage form by physisorption technique.

    Materials and methods: AZ was selected as an adsorbent and titanium dioxide nanoparticles as adsorbate. The AZ nanohybrids (AZN) were prepared by treating fixed amount of adsorbent with a varied amount of adsorbate, prepared separately by dispersing it in an aqueous medium. The mixture was sonicated, stirred followed by filtration and drying. The AZN produced were characterized by various techniques including scanning electron microscopy (SEM), energy dispersive X-rays (EDX), powder X-ray diffraction (PXRD), HPLC and Fourier-transformed infrared (FTIR). The optimized nanohybrid was blended with other excipients to get stable and taste masked dry suspension dosage form.

    Results: The results confirmed the adsorption of titanium dioxide nanoparticles on the surface of AZ. The fabricated optimized formulation was subjected for taste masking by panel testing and accelerated stability studies. The results showed a remarkable improvement in bitter taste masking, inhibiting throat bite without affecting the dissolution rate. The product showed an excellent stability both in dry and reconstituted suspension. The optimized formulation of AZN and was found stable when subjected to physical and chemical stability studies, this is because of short and single step process which interns limits the exposure of the product to various environmental factors that could potentially affect the stability of the product. The dissolution rate of the optimized formulation of AZN was compared with its marketed counterpart, showing the same dissolution rate compared to its marketed formulation.

    Conclusion: The current study concludes that, by fabricating AZ-titanium nanohybrids using physisorption can effectively mask the bitter taste of the drug. The palatability and stability of azithromycin formulation was potentially enhanced without affecting its dissolution rate.

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