SYNTHESIS AND EVALUATION OF WATER-SOLUBLE INDOLE PYRROLOTHIAZOLE PAF ANTAGONISTS

被引：5
|
作者：
SHEPPARD, GS
DAVIDSEN, SK
CARRERA, GM
PIREH, D
HOLMS, JH
HEYMAN, HR
STEINMAN, DH
CURTIN, ML
CONWAY, RG
RHEIN, DA
ALBERT, DH
TAPANG, P
MAGOC, TJ
SUMMERS, JB
机构：
[1] Immunosciences Research Area, Department 47J, Abbott Laboratories, Abbott Park, IL 60064
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 23期
关键词：
D O I：
10.1016/0960-894X(95)00511-Q
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
3-(3-Pyridinyl)-7-(indol-3-ylcarbonyl)-1H-3H-pyrrolo[1,2-c] thiazoles represent a class of potent, orally active PAF antagonists; however, the lead compounds in this series suffered from a lack of aqueous solubility. To overcome this limitation, a number of strategies were examined to achieve improved solubility, involving the incorporation of polar substituents and the use of prodrugs.
引用
收藏
页码：2913 / 2918
页数：6
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