苯腙基吲哚啉酮和糖基化 1,2,3-三唑基甲基吲哚啉-2,3-二酮的糖缀合物杂合的合成及抗疟活性。
Synthesis and antiplasmodial activity of glyco-conjugate hybrids of phenylhydrazono-indolinones and glycosylated 1,2,3-triazolyl-methyl-indoline-2,3-diones.
机构信息
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
Parasitology Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
出版信息
Eur J Med Chem. 2018 Jul 15;155:764-771. doi: 10.1016/j.ejmech.2018.06.042. Epub 2018 Jun 19.
A small library of 36 new glycohybrids of phenylhydrazono-indolinones was synthesized employing glycosylated 1,2,3-triazolyl-methyl-indoline-2,3-diones and different phenylhydrazines via acid catalyzed reaction. All the compounds were screened for their antiplasmodial activity in vitro. Compounds 6c, 7c, and 7b showed significant activity with the IC values 1.27, 1.64 and 1.96 μM, respectively against CQ sensitive Pf3D7 strain while compounds 7b and 6f showed good activity with IC 1.61 and 1.93 μM, respectively against CQ resistant PfK1 strain.
采用糖基化 1,2,3-三唑基-甲基-吲哚啉-2,3-二酮和不同的苯肼，通过酸催化反应合成了 36 种新的苯腙基-吲哚啉酮糖基杂合物的小文库。所有化合物均在体外进行抗疟活性筛选。化合物 6c、7c 和 7b 对 CQ 敏感 Pf3D7 株的 IC 值分别为 1.27、1.64 和 1.96μM，表现出显著的活性，而化合物 7b 和 6f 对 CQ 耐药 PfK1 株的 IC 值分别为 1.61 和 1.93μM，表现出良好的活性。
Zotero 插件