4.1 Article

Heterocycles in drugs and drug discovery

Journal

CHEMISTRY OF HETEROCYCLIC COMPOUNDS
Volume 48, Issue 1, Pages 7-10

Publisher

SPRINGER
DOI: 10.1007/s10593-012-0960-z

Keywords

bioisosteres; ClogP; drug discovery; heterocycles; hydrogen bonding; lipophilicity; polarity; PSA; TPSA

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Heterocycles are common fragments of the vast majority of marketed drugs. This is a reflection of the central role that heterocycles play in modern drug design. They can serve as useful tools to manipulate lipophilicity, polarity, and hydrogen bonding capacity of molecules, which may lead to improved pharmacological, pharmacokinetic, toxicological, and physicochemical properties of drug candidates and ultimately drugs.

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