Suppr超能文献

噻唑/噁唑取代苯并噻唑衍生物的合成、抗炎和镇痛评价。

Synthesis, anti-inflammatory and analgesic evaluation of thiazole/oxazole substituted benzothiazole derivatives.

机构信息

Department of Chemistry, Krishna College, Bijnor 246701, UP, India.

Department of Chemistry, Deen Dayal Upadhyaya Gorakhpur University, Gorakhpur 273009, UP, India.

出版信息

Bioorg Chem. 2021 Feb;107:104608. doi: 10.1016/j.bioorg.2020.104608. Epub 2020 Dec 31.

Abstract

Non-Steroidal biologically active heterocyclic compounds 4-(2-(4-chlorophenyl) benzo[d]thiazol-3(2H)-yl)-N-((3-substituted-2-hydrobenzo[d]thiazol-2-yl)methylene) thiazol-2-amine (3a-3d), 4-(2-(4-chlorophenyl)benzo[d]thiazol-3(2H)-yl)-N-((3-substituted - 2-hydrobenzo [d]thiazol-2-yl)methylene)oxazol-2-amine (3a'-3d'), (Z)-N'-(4-(2-(4-chlorophenyl)benzo[d]thiazol-3(2H)-yl)thiaol-2-yl)-N-(4-substituted phenylimino)-3-substituted-2-hydrobenzo[d]thiazole-2-carboxamidine (4a-4 h) and (Z)-N'-(4-(2-(4-chlorophenyl)benzo[d]thiazol-3(2H)-yl)oxazol-2-yl)-N-(4-substituted phenylimino) - 3-substituted-2-hydrobenzo[d]thiazole-2-carboxamidine (4a'-4h') were synthesized starting from 2-chloro-1-(2-(4-chlorophenyl)benzo[d]thiazol-3(2H)-yl) ethanone (1). The structure configuration of newly synthesized compounds has been determined by elemental analysis and various spectroscopic (IR, HNMR and GCMS) techniques. These compounds were tested for their anti-inflammation, analgesic, ulcerogenic, acute toxicity and free radical scavenging action and compared with reference drugs in albino rats. Compound 4-(2-(4-chlorophenyl)benzo[d]thiazol-3(2H)-yl)-N-((3-substituted-2-hydrobenzo [d]thiazol-2-yl)methylene)thiazol-2-amine (3c) was the most active compound than reference drug at a dose of 50 mg/kg p.o.

摘要

非甾体生物活性杂环化合物 4-(2-(4-氯苯基)苯并[d]噻唑-3(2H)-基)-N-((3-取代-2-羟苯并[d]噻唑-2-基)亚甲基)噻唑-2-胺 (3a-3d)、4-(2-(4-氯苯基)苯并[d]噻唑-3(2H)-基)-N-((3-取代-2-羟苯并[d]噻唑-2-基)亚甲基)恶唑-2-胺 (3a'-3d')、(Z)-N'-(4-(2-(4-氯苯基)苯并[d]噻唑-3(2H)-基)硫代-2-基)-N-(4-取代苯基亚氨基)-3-取代-2-羟苯并[d]噻唑-2-甲脒 (4a-4h) 和 (Z)-N'-(4-(2-(4-氯苯基)苯并[d]噻唑-3(2H)-基)恶唑-2-基)-N-(4-取代苯基亚氨基)-3-取代-2-羟苯并[d]噻唑-2-甲脒 (4a'-4h') 是从 2-氯-1-(2-(4-氯苯基)苯并[d]噻唑-3(2H)-基)乙酮 (1) 开始合成的。新合成化合物的结构构型已通过元素分析和各种光谱 (IR、HNMR 和 GCMS) 技术确定。这些化合物在白化大鼠中进行了抗炎、镇痛、溃疡形成、急性毒性和自由基清除作用的测试,并与参比药物进行了比较。化合物 4-(2-(4-氯苯基)苯并[d]噻唑-3(2H)-基)-N-((3-取代-2-羟苯并[d]噻唑-2-基)亚甲基)噻唑-2-胺 (3c) 在 50mg/kg po 剂量下比参比药物更具活性。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验