Hadjipavlou-Litina D J, Geronikaki A A
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Greece.
Drug Des Discov. 1998 May;15(3):199-206.
Several thiazolyl derivatives are reported to act as lipoxygenase inhibitors affecting inflammation and/or psoriasis. Two series of new thiazolyl and benzothiazolyl Schiff bases have been designed, synthesized and identified. RM values were determined as an expression of lipophilicity. The compounds were screened for their reducing activity (with the stable free radical 1,1-diphenyl-2-picrylhydrazyl DPPH), for radical scavenging activity (with the xanthine/xanthine oxidase system for O2.-) and for inhibition of soybean lipoxygenase (LO). Anti inflammatory activity was examined in vivo, using the carrageenin induced mice paw edema (24-71.8% inhibition was observed). The results are discussed in terms of structural and physicochemical characteristics of the compounds. Comparing the results among all tests, the benzothiazolyl derivatives seem to be more potent.
据报道，几种噻唑基衍生物可作为脂氧合酶抑制剂，影响炎症和/或银屑病。已设计、合成并鉴定了两个系列的新型噻唑基和苯并噻唑基席夫碱。测定RM值作为亲脂性的一种表达。对这些化合物进行了还原活性（用稳定自由基1,1-二苯基-2-苦基肼DPPH）、自由基清除活性（用黄嘌呤/黄嘌呤氧化酶系统检测O2-）和大豆脂氧合酶（LO）抑制活性的筛选。在体内使用角叉菜胶诱导的小鼠爪肿胀模型检测抗炎活性（观察到24 - 71.8%的抑制率）。根据化合物的结构和物理化学特性对结果进行了讨论。比较所有测试的结果，苯并噻唑基衍生物似乎更有效。
