Synthesis and in vitro Trichomonacidal activities of some new dialkylperoxides and 1,2,4-trioxanes

被引：24

作者：

Camuzat-Dedenis, B

Provot, O ^{[1
]}

Cointeaux, L

Perroux, V

Berrien, JF

Bories, C

Loiseau, PM

Mayrargue, JL

机构：

[1] Fac Pharm Chatenay Malabry, Chim Organ Lab, BioCIS, ESA 8076, F-92296 Chatenay Malabry, France

[2] Fac Pharm Chatenay Malabry, Parasitol Lab, EA 398, F-92296 Chatenay Malabry, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 36卷 / 10期

关键词：

peroxides; Trichomonas vaginalis; metronidazole; tiroxanes;

D O I：

10.1016/S0223-5234(01)01278-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two series of three trioxanes and 18 disubstituted peroxides were synthesised and evaluated for their in vitro trichomonacidal activity against Trichomonas vaginalis. The most active compound. 2-methylprop-2-yl 2-methoxyeth-1-yl peroxide exhibited an IC50 value of 1.0+/-0.2 muM whereas other dialkyl peroxides had various IC50 values which could not be correlated to their molecule structure. The best compound was about five times more active than metronidazole. The amount of generated oxygen or free radicals cannot explain completely the activity suggesting another way of action for these compounds on T. vaginalis. (C) 2001 Editions scientifiques et medicales Elsevier SAS.

引用

页码：837 / 842

页数：6

共 16 条

[1]

BURGEOIS M, 1989, SYNTHESIS-STUTTGART, V9, P700

[2] Alkylating properties of synthetic trioxanes related to artemisinin [J].