N-烷基脒的氨基甲酸酯前药。

Carbamate prodrugs of N-alkylfuramidines.

作者信息

Rahmathullah Syed M, Tidwell Richard R, Jones Susan K, Hall James E, Boykin David W

机构信息

Department of Chemistry, Georgia State University, University Plaza, Atlanta, GA 30303-3082, United States.

出版信息

Eur J Med Chem. 2008 Jan;43(1):174-7. doi: 10.1016/j.ejmech.2007.03.009. Epub 2007 Apr 3.

DOI:10.1016/j.ejmech.2007.03.009

PMID:17499888

Abstract

The synthesis and evaluation of 2,5-bis[4-(N-ethoxycarbonyl-N'-isopropyl)amidinophenyl]furan, 2,5-bis[4-(N-2,2,2-trichloroethoxycarbonyl-N'-isopropyl)amidinophenyl]furan and 2,5-bis[4-(N-cyclopentyl-N'-2,2,2-trichloroethoxycarbonyl)amidinophenyl]furan as prodrugs of bis-N-alkylamidines are reported. The results show that the bis-2,2,2-trichloroethyl carbamates function effectively in a rat model for Pneumocystis pneumonia.

摘要

报道了2,5-双[4-(N-乙氧基羰基-N'-异丙基)脒基苯基]呋喃、2,5-双[4-(N-2,2,2-三氯乙氧基羰基-N'-异丙基)脒基苯基]呋喃和2,5-双[4-(N-环戊基-N'-2,2,2-三氯乙氧基羰基)脒基苯基]呋喃作为双-N-烷基脒前药的合成与评价。结果表明，双-2,2,2-三氯乙基氨基甲酸酯在卡氏肺孢子虫肺炎大鼠模型中发挥了有效的作用。