Bioisosteric equivalence of five-membered heterocycles

被引：10
|
作者：
Dudkin, V. Y. [1 ]
机构：
[1] Merck Res Labs, Dept Med Chem, West Point, PA 18486 USA
来源：
CHEMISTRY OF HETEROCYCLIC COMPOUNDS | 2012年 / 48卷 / 01期
关键词：
heterocycles; bioisosterism; lead optimization; medicinal chemistry; scaffold hopping; CENTER-DOT-O; DRUG DESIGN; KINASE INHIBITORS; HYDROGEN-BONDS; KDR KINASE; POTENT; REPLACEMENT; DISCOVERY;
D O I：
10.1007/s10593-012-0964-8
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A variety of factors can affect bioisosteric relationships between structural motifs in a medicinal chemistry optimization project, both in terms of ligand affinity to a given target and off-target profile. Such parameters, e.g. the ability to participate in hydrogen bonding and pi-pi interactions, basicity, and solubility are discussed with a particular focus on five-membered heterocycles and their application in drug design.
引用
收藏
页码：27 / 32
页数：6
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