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1,2,4-三唑并[3,4-b]1,3,4-噻二唑及其二氢类似物的合成与药理活性研究

Studies on synthesis and pharmacological activities of 1,2,4-triazolo[3,4-b]1,3,4-thiadiazoles and their dihydro analogues.

作者信息

Mathew Vinod, Giles Devasahayam, Keshavayya Jathi, Vaidya Vijaya P

机构信息

Acharya & B. M. Reddy College of Pharmacy, Department of Pharmaceutical Chemistry, Bangalore, Karnataka, India.

出版信息

Arch Pharm (Weinheim). 2009 Apr;342(4):210-22. doi: 10.1002/ardp.200800073.

Abstract

4-Amino-5-substituted aryl-3-mercapto-1,2,4-triazoles are versatile synthons for constructing various biologically active heterocycles. Starting from 4-amino-5-substituted aryl-3-mercapto-1,2,4-triazole 3a-c, a series of new 3,5-disubstituted-1,2,4-triazolo-[3,4-b]1,3,4-thiadiazoles and their 5,6-dihydrotriazolothiadiazoles were prepared. The structures of all the newly synthesized compounds have been confirmed by elemental analysis, IR,( 1)H-NMR, (13)C-NMR, and mass spectra. The antimicrobial effects of the synthesized compounds were investigated using the paper disc method. Anti-inflammatory and analgesic activities of the synthesized compounds were assessed by carrageenan-induced rat paw oedema method and by Eddy's hot plate method, respectively. Some of the compounds exhibited promising antimicrobial activities as well as moderate to good anti-inflammatory activity and analgesic activity.

摘要

4-氨基-5-取代芳基-3-巯基-1,2,4-三唑是用于构建各种生物活性杂环的通用合成子。从4-氨基-5-取代芳基-3-巯基-1,2,4-三唑3a-c出发,制备了一系列新的3,5-二取代-1,2,4-三唑并[3,4-b]1,3,4-噻二唑及其5,6-二氢三唑并噻二唑。所有新合成化合物的结构均已通过元素分析、红外光谱、(1)H-NMR、(13)C-NMR和质谱确证。采用纸片法研究了合成化合物的抗菌效果。分别通过角叉菜胶诱导的大鼠足肿胀法和Eddy热板法评估了合成化合物的抗炎和镇痛活性。部分化合物表现出良好的抗菌活性以及中度至良好的抗炎和镇痛活性。

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