Antileishmanial dinitroaniline sulfonamides with activity against parasite tubulin
Antileishmanial dinitroaniline sulfonamides with activity against parasite tubulin
复制标题
DOI：
10.1016/s0960-894x(02)00465-1
复制
发表时间：
2002-09-02
影响因子：
2.7
通讯作者：
Werbovetz, KA
中科院分区：
文献类型：
--
作者：
Bhattacharya, G;Salem, MM;Werbovetz, KA
以除草剂oryzalin 3为基础合成了新型二硝基苯胺类磺胺类除草剂，并测定了其对寄生原生动物利什曼多诺瓦原虫和利什曼微管蛋白的抑制活性。这些化合物的一个子集在体外对利什曼原虫和靶蛋白都具有更强的活性。化合物20对利什曼微管蛋白的抑制活性较oryzalin高13.4倍，对L. donovani axenic amastigotes的抑制活性较oryzalin高。(C) 2002 Elsevier Science Ltd.版权所有。
Novel dinitroaniline sulfonamides based on the herbicide oryzalin 3 were synthesized and evaluated for activity against the parasitic protozoan Leishmania donovani and against leishmanial tubulin, the putative antiparasitic target of oryzalin. A subset of these compounds possess more activity against both Leishmania and the target protein in vitro. Compound 20 displays improved potency against leishmanial tubulin and is 13.4-fold more active against L. donovani axenic amastigotes than oryzalin. (C) 2002 Elsevier Science Ltd. All rights reserved.