噻唑基和苯并噻唑基席夫碱作为可能的新型脂氧合酶抑制剂和抗炎剂。合成和生物学评价。

Drug design and discovery Pub Date : 1998-05-01
D J Hadjipavlou-Litina, A A Geronikaki
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引用次数: 0

摘要

据报道,几种噻唑基衍生物可作为影响炎症和/或牛皮癣的脂氧合酶抑制剂。我们设计、合成并鉴定了两个系列的新噻唑基和苯并噻唑基席夫碱。RM 值被确定为亲脂性的一种表现形式。筛选了这些化合物的还原活性(使用稳定自由基 1,1-二苯基-2-苦基肼 DPPH)、自由基清除活性(使用黄嘌呤/黄嘌呤氧化酶系统清除 O2.-)以及对大豆脂氧合酶 (LO) 的抑制作用。利用角叉菜胶诱发的小鼠爪水肿对其体内的抗炎活性进行了检测(观察到 24%-71.8% 的抑制作用)。研究结果从化合物的结构和理化特性方面进行了讨论。比较所有试验的结果,苯并噻唑衍生物似乎更有效。
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Thiazolyl and benzothiazolyl Schiff bases as novel possible lipoxygenase inhibitors and anti inflammatory agents. Synthesis and biological evaluation.

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.

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