Antimalarial and cytotoxic activities of chiral triamines
Antimalarial and cytotoxic activities of chiral triamines
复制标题
DOI：
10.1016/j.bmcl.2013.06.035
复制
发表时间：
2013-08-15
影响因子：
2.7
通讯作者：
Nefzi, Adel
中科院分区：
文献类型：
--
作者：
Dellai, Afef;Appel, Jon;Nefzi, Adel
在筛选由31，320种抗恶性疟原虫的化合物组成的基于混合物的位置扫描文库后，已鉴定出手性三胺抗疟化合物。在彻底还原树脂结合的酰化二肽后生成文库，即N-甲基三胺（TPI 762）。使用PSCL方法，快速鉴定出活性仅比标准药物氯喹（CQ）和青蒿素（阿尔特斯）低10倍的单个化合物。(C)2013爱思唯尔有限公司保留所有权利。
Chiral triamine antimalarial compounds have been identified following the screening of mixture-based positional scanning libraries made up of 31,320 compounds against P. falciparum. The library, namely N-methyl triamine (TPI 762) was generated following exhaustive reduction of resin-bound acylated dipeptides. Using the PSCL approach, individual compounds were rapidly identified which were only 10 times less active than the standard drugs chloroquine (CQ) and Artemisinin (Artes). (C) 2013 Elsevier Ltd. All rights reserved.