Artemisinin tricyclic analogs:: Role of a methyl group at C-5a

被引:18
|
作者
Zouhiri, F
Desmaële, D
d'Angelo, J
Riche, C
Gay, F
Cicéron, L
机构
[1] Univ Paris Sud, Ctr Etud Pharmaceut, Unite Chim Organ, CNRS, F-92296 Chatenay Malabry, France
[2] CNRS, Inst Chim Subst Nat, F-91198 Gif Sur Yvette, France
[3] Grp Hosp Pitie Salpetriere, Lab Epidemiol & Chimioresistance Paludisme, Serv Parasitol, F-75651 Paris, France
关键词
antiprotozoals; trioxanes; silicon and compounds; ozonolysis;
D O I
10.1016/S0040-4039(98)00390-6
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
New artemisinin tricyclic analogs, bearing a methyl group at C-5a were synthetized through ozonation of vinylsilanes. Presence of such a substituent was detrimental to the antimalarial activity of these trioxanes, thus reinforcing the hypothesis that tight hemin-trioxane complexes are involved in the activation phase of these compounds. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2969 / 2972
页数:4
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