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 …

Isosteric replacement of amide groups is a classic practice in medicinal chemistry. This
digest highlights the applications of most commonly employed amide isosteres in drug …

The concept of isosterism between relatively simple chemical entities was originally
contemplated by James Moir in 1909, a notion further refined by HG Grimm's hydride …

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 …

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 …

One of the key challenges for the medicinal chemist today is the modulation and mediation
of the potency of a small-molecule therapeutic against its biological target. In addition, it is …

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 …

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 …

Allostery is the most direct and efficient way for regulation of biological macromolecule
function, ranging from the control of metabolic mechanisms to signal transduction pathways …

Years of cumulative research can result in the development of a clinically useful drug,
providing either a cure for a particular disease or symptomatic relief from a physiological …