Lead optimization represents the tedious process of fine‐tuning lead compounds from
biologically active hits to suitable drug candidates for clinical trials. By chemically modifying …

Background: The carboxylic acid moiety is an important functional group which features in
the pharmacophore of some 450 drugs. Unfortunately, some carboxylic acid-containing …

The carboxylic acid functional group can be an important constituent of a pharmacophore,
however, the presence of this moiety can also be responsible for significant drawbacks …

Drug design is a complex process that requires a good command of several disciplines
including organic and physical chemistry, biochemistry and metabolism, pharmacology …

The benzene moiety is the most prevalent ring system in marketed drugs, underscoring its
historic popularity in drug design either as a pharmacophore or as a scaffold that projects …

The amide functional group plays a key role in the composition of biomolecules, including
many clinically approved drugs. Bioisosterism is widely employed in the rational …

Bioisosterism: A Useful Strategy for Molecular Modification and Drug Design Page 1 Current
Medicinal Chemistry, 2005, 12, 23-49 23 0929-8673/05 $50.00+.00 © 2005 Bentham Science …

Exposing the importance of the carboxylic acid functional group is best achieved by
examining the number of endogenous processes and individual molecules which rely on the …

Publisher Summary This chapter discusses the use of bioisosteric groups in lead
optimization. The concept of bioisosteres refers to compounds or a substructure of …

It is now half a century since Friedman introduced the term bioisosterism for the similar
biological activity of structurally related compounds. Since then, the concept has been used …