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 …

A quaternary carbon bears four other carbon substituents or combination of four non-
hydrogen substituents at four vertices of a tetrahedron. The spirocyclic quaternary carbon …

There is increasing interest in replacement of the planar aromatic rings of drug candidates
with three-dimensional caged scaffolds in order to improve the physical properties, but …

Abstract Bicyclic hydrocarbons, and bicyclo [1.1. 1] pentanes (BCPs) in particular, are
playing an emerging role as saturated bioisosteres in pharmaceutical, agrochemical and …

Highly strained 1, 3-disubstituted bicyclo [1.1. 1] pentanes (BCPs) have been established as
bioisosteres of para-disubstituted benzene because they impart valuable pharmacokinetic …

The design of bioisosteres represents a creative and productive approach to improve a
molecule, including by enhancing potency, addressing pharmacokinetic challenges …

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 …

Modular functionalization enables versatile exploration of chemical space and has been
broadly applied in structure–activity relationship (SAR) studies of aromatic scaffolds during …

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 …

Abstract The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of
the key properties of over 2000 human drug targets with their pharmacology, plus links to an …