Synthesis and in vitro and in vivo antimalarial activity of N 1-(7-chloro-4-quinolyl)-1, 4-bis (3-aminopropyl) piperazine derivatives

…, E Mouray, P Grellier, C Sergheraert

文献索引：Girault, Sophie; Grellier, Philippe; Berecibar, Amaya; Maes, Louis; Mouray, Elisabeth; Lemiere, Pascal; Debreu, Marie-Ange; Davioud-Charvet, Elisabeth; Sergheraert, Christian Journal of Medicinal Chemistry, 2000 , vol. 43, # 14 p. 2646 - 2654

全文：HTML全文

被引用次数: 99

摘要

Three series of monoquinolines consisting of a 1, 4-bis (3-aminopropyl) piperazine linker and a large variety of terminal groups were synthesized. Our aim was to prove that in related bisquinoline, it is the second quinoline moiety that is responsible for cytotoxicity and that it is not an absolute requirement for overcoming resistance to chloroquine (CQ). Eleven compounds displayed a higher selectivity index (ratio CC50/IC50 activity) than CQ, and ...