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SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY OF POLYKETONES

Chinese Journal of Polymer Science 2013年第3期31卷 471-480页

作者： Ismail A.Alkskas Altaher M.Alhubge faizul azam Polymer Lab Department of ChemistryFaculty of ScienceMisurata University Department of Microbiology Faculty of ScienceMisurata University Faculty of Pharmacy Misurata University

Polyketone resins have been prepared by the Friedel-Crafts polymerization of dithiophenylidenecyclopentanone （I）, dithiophenylidenecyclohexanone （II） and dithiophenylideneacetone （III） with adipoyl, sebacoyl and terephthaloyl dichlorides using boron trifluoride as catalyst and carbon disulphide as solvent. Polymers were characterized with IR, 1H- NMR, and the results showed the presence of carbonyl of ketonic groups in the main chain. The polyketones have inherent viscosities of 0.40-0.70 dL/g. All the polymers are semicrystalline and most of them are partially soluble in most common organic solvents but freely soluble in aprotic solvents. The temperatures of 50% weight loss are as high as 185℃ to 280℃ in air, indicating that these aromatic polyketones have excellent thermal stability. All the polyketones were tested for their antimicrobial activity against bacteria and fungi.

关键词： Synthesis Characterization Polyketones Biological activity.

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Synthesis and Characterization of Polyesters Based on Diethylketone Moiety

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Chinese Journal of Polymer Science 2014年第11期32卷 1450-1459页

作者： Ismail A.Alkskas Bashir A.El-gnidi Khadija M.Ghalieo faizul azam Polymer Lab Department of ChemistryFaculty of ScienceMisurata University Faculty of Pharmacy Misurata University

A new class of unsaturated polyesters based on diethylketone have been prepared by interfacial polymerization of 2,4-bis（4-hydroxybenzylidene）-3-pentanone（I） and 2,4-bis（4-hydroxy-3-methoxybenzylidene）-3-pentanone（II） with 4,4’-azodibenzoyl chloride and 3,3’-azodibenzoyl chloride at ambient temperature. The model compounds were synthesized by reaction of（I） and（II） with benzoyl chloride. The new monomers, model compounds and polyesters have been characterized by different spectral analyses. The polyesters have inherent viscosity of 0.55-0.80 d L/g and moderate number average molecular weight（Mn） in the range of 6150-7400 g/mol. Most of the compounds exhibited their solubility in aprotic solvents while partial solubility in various halogenated organic solvents was observed. The temperatures of 10% weight loss were high（225-330 °C） in nitrogen, indicating that these polyesters have excellent thermal stability. Doping with iodine dramatically raised the conductivity and produced brown colored semiconductive polymers with a maximum conductivity of 2.7 × 10-6 --1cm-1. Moreover, the morphological properties of selected example of polyesters were detected by SEM.

关键词： Diethylketone Azo Polyesters Conductivity.

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Synthesis of Schiff bases of naphtha[1,2-d]thiazol-2-amine and metal complexes of 2-(2'-hydroxy)benzylideneaminonaphthothiazole as potential antimicrobial agents

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Journal of Zhejiang University-Science B(Biomedicine & Biotechnology) 2007年第6期8卷 446-452页

作者： azam faizul SINGH Satendra KHOKHRA Sukhbir Lal PRAKASH Om Department of Pharmaceutical Sciences Kurukshetra University Kurukshetra Haryana 136119 India Faculty of Pharmacy Seventh of October University P.O. Box 2909 Misurata Libya B. R. Ambedkar Center for Biomedical Research University of Delhi Delhi 110007 India Dr. Department of Pharmaceutical Sciences Kurukshetra University Kurukshetra Haryana 136119 India

Objective： A series of 2-benzylideneaminonaphthothiazoles were designed and synthesized incorporating the lipophilic naphthalene ring to render them more capable of penetrating various biomembranes. Methods： Schiff bases were synthesized by the reaction of naphtha[1,2-d]thiazol-2-amine with various substituted aromatic aldehydes. 2-（2＇-Hydroxy）ben- zylideneaminonaphthothiazole was converted to its Co（Ⅱ）, Ni（Ⅱ） and Cu（Ⅱ） metal complexes upon treatment with metal salts in ethanol. All the compounds were evaluated for their antibacterial activities by paper disc diffusion method with Gram positive Staphylococcus aureus and Staphylococcus epidermidis and Gram negative Escherichia coli and Pseudomonas aeruginosa bacteria. The minimum inhibitory concentrations of all the Schiff bases and metal complexes were determined by agar streak dilution method. Results： All the compounds moderately inhibited the growth of Cram positive and Gram negative bacteria. In the present study among all Schiff bases 2-（2＇-hydroxy）benzylideneaminonaphthothiazole showed maximum inhibitory activity and among metal complexes Cu（Ⅱ） metal complex was found to be most potent. Conclusion： The results obtained validate the hypothesis that Schiff bases having substitution with halogens, hydroxyl group and nitro group at phenyl ring are required for the antibacterial activity while methoxy group at different positions in the aromatic ring has minimal role in the inhibitory activity. The results also indicated that the metal complexes are better antibacterial agents as compared to the Schiff bases.

关键词： Schiff bases Metal complexes Antimicrobial

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Nigella sativa oil alleviates doxorubicin-induced cardiomyopathy and neurobehavioral changes in mice:In vivo and in-silico study

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Asian Pacific Journal of Tropical Biomedicine 2022年第7期12卷 312-322页

作者： Md Jamir Anwar Sattam Khulaif Alenezi faizul azam Danish Mahmood Faisal Imam Khalid Saad Alharbi Department of Pharmacology and Toxicology Unaizah College of PharmacyQassim UniversityAl-QassimSaudi Arabia Department of Pharmaceutical Chemistry&Pharmacognosy Unaizah College of PharmacyQassim UniversityAl-QassimSaudi Arabia Department of Pharmacology and Toxicology College of PharmacyKing Saud UniversityRiyadhSaudi Arabia Department of Pharmacology College of PharmacyJouf UniversitySakakahSaudi Arabia

Objective:To investigate the effect of Nigella sativa oil on cardiomyopathy and neurobehavioral changes induced by doxorubicin in ***:Swiss strain of albino female mice were divided into 6 groups of 5 animals in each:GroupⅠ(control group),groupⅡ(doxorubicin,10 mg/kg,i.v.),groupⅢ,Ⅳ,andⅤ(Nigella sativa oil;1.5,3,and 6 mL/kg,respectively),groupⅥ(Nigella sativa oil per se;6 mL/kg,p.o.).The duration of treatment was 15 d(10 days’pre-treatment and 5 days’post-treatment)and doxorubicin was administered on day 11th of the treatment *** Nigella sativa oil treatment,neurobehavioral tests,cardiac hypertrophy tests,and biochemical tests in serum and tissues were *** tests included assessment of anxiety-like behavior in the elevated plus maze,spontaneous alternation behavior in the cross maze,and depression-like behavior in modified forced swim *** tests included serum lactate dehydrogenase and creatinine kinase-MB,malondialdehyde and reduced glutathione in ***,molecular docking was used to estimate the affinity of the phytoconstituents of Nigella sativa oil with histone ***:Nigella sativa oil treatment significantly(P<0.001)restored doxorubicin-induced neurobehavioral changes,decreased lactate dehydrogenase and creatinine kinase-MB in the plasma,malondialdehyde contents in tissues,and increased reduced glutathione ***,no significant alteration was observed in Nigella sativa oil per se group as compared to the *** docking showed that Nigella sativa oil components had appreciable binding affinitiy with the protein cavities of HDAC1 and ***:The result shows that Nigella sativa oil exerts anxiolytic,antidepressant,and memory-enhancing effects in addition to cardioprotective effect against doxorubicin-induced cardiomyopathy in *** modulatory effect of Nigella sativa oil on oxidative stress could contribute to the cardioprotective effect and associated neuro

关键词： Nigella sativa oil Doxorubicin Cardiomyopathy Neurobehavioral changes Lactate dehydrogenase Creatinine kinase-MB Malondialdehyde Reduced glutathione Mice HDAC docking

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