PHYSICAL PARAMETERS FOR BRAIN UPTAKE - OPTIMIZING LOG-P, LOG-D AND PKA OF THA

被引：21

作者：

DESAI, MC

THADEIO, PF

LIPINSKI, CA

LISTON, DR

SPENCER, RW

WILLIAMS, IH

机构：

[1] Central Research Division, Pfizer Inc., Groton

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1991年 / 1卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(00)80267-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two positions on the acetylcholinesterase (AChE) inhibitor, 9-amino-1,2,3,4-tetrahydroacridine (THA), have been identified which can be modified to vary log P, log D and pK(a) values. Most importantly, these changes can be carried out without altering its AChE activity.

引用

页码：411 / 414

页数：4

共 12 条

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