BIOISOSTERIC EQUIVALENCE OF FIVE-MEMBERED HETEROCYCLES

Авторы

  • V. Y. Dudkin Department of Medicinal Chemistry, Merck Research Laboratories

DOI:

https://doi.org/10.1007/1287

Ключевые слова:

heterocycles, bioisosterism, lead optimization, medicinal chemistry, scaffold hopping

Аннотация

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 π–π-interactions, basicity, and solubility are discussed with a particular focus on five-membered heterocycles and their application in drug design.

Also published in Chemistry of Heterocyclic Compounds, 2012, 48 (1), pp 27-32

http://link.springer.com/article/10.1007/s10593-012-0964-8

Загрузки

Опубликован

2013-12-04

Выпуск

№ 1 (2012)

Раздел

Обзорные статьи