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Synthesis, anti-inflammatory and analgesic evaluation of thiazole/oxazole substituted benzothiazole derivatives
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-12-31 , DOI: 10.1016/j.bioorg.2020.104608
Gajendra Kumar 1 , N P Singh 2
Affiliation  

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, 1HNMR 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.



中文翻译:

噻唑/恶唑取代苯并噻唑衍生物的合成、抗炎和镇痛评价

非甾体生物活性杂环化合物 4-(2-(4-chlorophenyl) benzo[ d ]thiazol-3(2H)-yl)-N-((3-located-2-hydrobenzo[ d ]thiazol-2-yl )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-取代的-2-氢苯并[ d] thiazol -2-yl)methylene) oxazol -2-amine (3a'-3d'), (Z)-N'-(4-(2-(4-chlorophenyl)benzo[ d ]thiazol-3(2H)) )-基)硫醇-2-基)-N-(4-取代苯基亚氨基)-3-取代-2-氢苯并[ 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-氢苯并[从 2-氯-1-(2-(4-氯苯基)苯并[ d ]噻唑-3(2H)-基)乙酮(1)开始合成d ]噻唑-2-甲脒(4a'-4h' )。新合成化合物的结构构型已通过元素分析和各种光谱(IR、1 HNMR 和 GCMS)技术确定。测试了这些化合物的抗炎、镇痛、致溃疡、急性毒性和自由基清除作用,并在白化大鼠中与参考药物进行了比较。化合物4-(2-(4-氯苯基)苯并[ d ]噻唑-3(2H)-基)-N-((3-取代-2-氢苯并[ d ]噻唑-2-基)亚甲基)噻唑-2 -胺(3c) 在 50 mg/kg po 的剂量下是比参比药物最具活性的化合物

更新日期:2021-01-18
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