کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2509401 1117663 2015 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and oral hypoglycemic effect of novel thiazine containing trisubstituted benzenesulfonylurea derivatives
ترجمه فارسی عنوان
سنتز و اثر هیپوگلیسمی دهانی تازین جدید حاوی مشتقات بنزن سولفونیل اوره
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی علوم دارویی
چکیده انگلیسی

A new series of 3-(4-substituted phenyl)-1-(4-(4,6-dimethyl-6H-1,3-thiazin-2-yl)phenylsulfonyl)-1-substituted urea (5a–o) was synthesized by an effectual route via sulfonylcarbamates and explores the novel site for substitution in sulfonylurea as well as the way of thiazine can be prepared. The molecules were established by elemental analysis and spectroscopic viz. IR, 1H NMR, 13C NMR and MS techniques. All the fifteen derivatives were shown very prominent oral hypoglycemic effect at the dose of 40 mg/kg body weight (p.o.) in respect of standard drug glibenclamide and control. The hypoglycemic effect was studied using oral glucose tolerance test in normal and NIDDM in STZ-rat model. The compounds 5a, 5d, 5f, 5i, 5k and 5n were dominant out of fifteen derivatives for blood glucose lowering activity (more than 80%) when comparing with NIDDM control. These derivatives were either containing simply phenyl ring (5a, 5f and 5k) on to the second amine of sulfonylurea (R′ = H) or nitro group at the para position in compound 5d, 5i and 5n (R′ = NO2) to produce significant oral hypoglycemic effect. Other structural activity relationship is also observed regarding the heteroaromatic and substituted aromatic group at R and R′ position respectively.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Saudi Pharmaceutical Journal - Volume 23, Issue 5, October 2015, Pages 475–482
نویسندگان
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