Department of Chemistry, Krishna College, Bijnor 246701, UP, India.
Department of Chemistry, Deen Dayal Upadhyaya Gorakhpur University, Gorakhpur 273009, UP, India.
Bioorg Chem. 2021 Feb;107:104608. doi: 10.1016/j.bioorg.2020.104608. Epub 2020 Dec 31.
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.
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。