کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8509062 | 1556008 | 2017 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis, characterization and pharmacological evaluation of different 1,3,4-oxadiazole and acetamide derivatives of ethyl nipecotate
ترجمه فارسی عنوان
سنتز، خصوصیات و ارزیابی فارماکولوژیک مشتقات مختلف 1،3،4-اکسیدیاازول و استامید نیتروژن
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کلمات کلیدی
1،3،4-اکادیازول، استامید، فعالیت ضد باکتری، فعالیت همولیتیک، مهار لیپوکسیژناز،
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
چکیده انگلیسی
A new series of N-substituted derivatives of 2-[(5-{1-[(4-chlorophenyl)sulfonyl]-3-piperidinyl}-1,3,4-oxadiazol-2-yl)sulfanyl]acetamide (6a-w) has been designed and synthesized with multifunctional moieties. The synthesized compounds were evaluated for their antibacterial and anti-enzymatic potential supported by % hemolytic activity. The synthesized compound 5-(1-(4-chlorophenylsulfonyl)-3-piperidinyl)-1,3,4-oxadiazole-2-thiol (3) was stirred with synthesized electrophiles as N-aryl/alkyl/aralkyl-2-bromoacetamide (5a-w) in an aprotic solvent under basic conditions to acquire the target molecules, 6a-w. The spectral analytical techniques of IR, EI-MS, 1H NMR and 13C-NMR were utilized for structural elucidation of synthesized molecules. The antibacterial screening against certain bacterial strains of gram-negative and gram-positive bacteria rendered compound 6i as good inhibitor of gram-negative bacterial strains. The enzyme inhibition revealed low potential against lipoxygenase (LOX) enzyme. The hemolytic study provided valuable information about cytotoxic behavior of synthesized molecules.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bulletin of Faculty of Pharmacy, Cairo University - Volume 55, Issue 2, December 2017, Pages 333-343
Journal: Bulletin of Faculty of Pharmacy, Cairo University - Volume 55, Issue 2, December 2017, Pages 333-343
نویسندگان
Khadija Nafeesa, Aziz-ur-Rehman Aziz-ur-Rehman, Muhammad A. Abbasi, Sabahat Z. Siddiqui, Shahid Rasool, Syed A.A. Shah,