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کاربرد نوع شرط:
- جایگاه : پژوهشی
- مجله: Iranian Journal of Basic Medical Sciences
- نوع مقاله: Journal Article
- کلمات کلیدی: acetylcholinesterase,coumarin,Alzheimer’s disease,Benzoheterocycles Butyrylcholinesterase
- چکیده:
- چکیده انگلیسی: Objective(s): To investigate the efficiency of a novel series of coumarin derivatives bearing benzoheterocycle moiety as novel cholinesterase inhibitors.
Materials and Methods: Different 7-hydroxycoumarin derivatives were synthesized via Pechmann or Knoevenagel condensation and conjugated to different benzoheterocycle (8-hydroxyquinoline, 2-mercaptobenzoxazole or 2-mercaptobenzimidazole) using dibromoalkanes 3a-m. Final compounds were evaluated against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) by Ellman's method. Kinetic study of AChE inhibition and ligand-protein docking simulation were also carried out for the most potent compound 3b.
Results: Some of the compounds revealed potent and selective activity against AChE. Compound 3b containing the quinoline group showed the best activity with an IC50 value of 8.80 µM against AChE. Kinetic study of AChE inhibition revealed the mixed-type inhibition of the enzyme by compound 3b. Ligand-protein docking simulation also showed that the flexibility of the hydrophobic five carbons linker allows the quinoline ring to form π-π interaction with Trp279 in the PAS.
Conclusion: We suggest these synthesized compounds could become potential leads for AChE inhibition and prevention of AD symptoms.- انتشار مقاله: 13-03-1396
- نویسندگان: Kimia Hirbod,Leili Jalili-baleh,Hamid Nadri,Seyed Esmaeil Sadat Ebrahimi,Alireza Moradi,Bahar Pakseresht,Alireza Foroumadi,Abbas Shafiee,Mehdi Khoobi
- مشاهده
- جایگاه : پژوهشی
- مجله: Iranian Journal of Chemistry and Chemical Engineering
- نوع مقاله: Journal Article
- کلمات کلیدی: 4-Hydroxycoumarin,Chalcones,Functionalized SBA-15,Pyrano[3,2-c]chromenones,Supported ionic liquid
- چکیده:
- چکیده انگلیسی: The surface of SBA-15 was modified by diphenylphosphine; then, it was treated with butane sultone and sulfuric acid to obtain Brønsted acid HO3S-phosphonium based ionic liquid functionalized SBA-15 with HSO4- as a counteranion. It efficiently catalyzed synthesis of pyrano[3,2-c]chromenone derivatives through the reaction of 4-hydroxycoumarin and chalcones at 60 °C in water/ethanol. Good yields, mild reaction conditions, and user-friendly procedure are advantages of this method. Also, the catalyst could be easily separated and reused five times without significant reduction of activity.
- انتشار مقاله: 28-02-1393
- نویسندگان: Mina Saeedi,Mohammad Jeiroudi,Leila Ma’mani,Mohammad Mahdavi,Eskandar Alipour,Abbas Shafiee,Ali Reza Foroumadi
- مشاهده
- جایگاه : پژوهشی
- مجله: Iranian Journal of Chemistry and Chemical Engineering
- نوع مقاله: Journal Article
- کلمات کلیدی: Synthesis,Vasicinone,Monobromodeoxyvasicinone,Acetylvasicinone
- چکیده:
- چکیده انگلیسی: A new, high yielding method for the preparation of vasicinone (7) is described. Reaction of 2-nitrobenzoic acid with N, N¢-carbonyldiimidazole followed by 2-pyrrolidinone gave 1-(2-nitrobenzoyl)pyrrolidine-2-one (3). Reduction of the latter with 10% Pd-C afforded deoxyvasicinone (4). Reaction of deoxyvasicinone (4) with bromine yielded monobromo-deoxyvasicinone (5). Exchange of bromine of 5 with acetoxy followed by hydrolysis gave vasicinone in high yield.
- انتشار مقاله: 26-07-1382
- نویسندگان: Vahid Ziaee,Hasan Jalalizadeh,Mehrdad Iranshahi,Abbas Shafiee
- مشاهده
- جایگاه : پژوهشی
- مجله: Iranian Journal of Chemistry and Chemical Engineering
- نوع مقاله: Journal Article
- کلمات کلیدی: essential oil,Antibacterial,Zataria multiflora,Antifungal,Labiatae
- چکیده:
- چکیده انگلیسی: The essential oils of Zataria multiflora (Labiatae) from four regions of Iran were investigated by GLC and GC-MS methods. The main constituents were carvacrol, thymol, linalool and p-cymene. The percentage of the constituents (in dry and wet plant) of different regions have been compared. Antibacterial and antifungal effects of these essential oils have been studied. The essential oil with highest percentage of thymol and carvacrol had a significant antimicrobial activity.
- انتشار مقاله: 31-06-1376
- نویسندگان: Abbas Shafiee,Katayon Javidnia,Mojtaba Tabatabai
- مشاهده
- جایگاه : پژوهشی
- مجله: Iranian Journal of Chemistry and Chemical Engineering
- نوع مقاله: Journal Article
- کلمات کلیدی: Beta-diketones,Nitroimidazole,Imidazolide,Isoxazoles,Isoxazoline
- چکیده:
- چکیده انگلیسی: The beta0diketone derivatives of nitroimidazole were synthesized from the reaction of magnesium salt of beta-ketoaccids 3 with imidazolide 4. The raction of beta-diketones with hydroxylamine hydrochloride afforded either the isoxazoles or the 5-hydroxyl-2-isoxazolines.
- انتشار مقاله: 21-02-1376
- نویسندگان: Abbas Shafiee,Mohammad ALi Ebrahimzadeh
- مشاهده
- جایگاه : پژوهشی
- مجله: Iranian Journal of Chemistry and Chemical Engineering
- نوع مقاله: Journal Article
- کلمات کلیدی: Antibacterial activity,Triazole,thiazole
- چکیده:
- چکیده انگلیسی: Starting from readily available 2-substituted-4-methylthiazole-5-carboxylic acid hydrazide (1), The title compounds were prepared. The reaction of compound 1 (R=CH3) with formic acid yielded 1-(formyl)-2-(2,4-dimethylthiazole-5-carboxyl) hydrazine (2). Refluxing the latter with phosphorous pentasulfide in xylene afforded compound 3, the reaction of compound 2 with phosphorous pentoxide afforded compound 4. Reaction of compound 1 with substituted isothiocyanates followed by cyclization of the intermediate 5 in basic medium gave 4-alkyl-5-(2-substituted-4-methyl-5-thiazolyl)-,4-dihydro-3H-1,2,4-triazole-3-thione (6). Alkylation of compound 6 followed by subsequent oxidation of intermediate 7 gave compound 8. The reaction of acid chloride 11 with hydrazide 12 afforded compound 13 which was cyclized by P2S5 to compounds 14 or 15 respectively. Compounds 3 and 14 showed significant activities against E. Coli and Bacillus Subtilis.
- انتشار مقاله: 23-07-1375
- نویسندگان: Abbas Shafiee,Amir Reza Jalilian,Mojtaba Tabatabaiee Yazdi
- مشاهده