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 …

Introduction There continues to be an exponential rise in the number of small molecule
drugs that contain either a fluorine atom or a fluorinated fragment. While the unique …

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 electronic properties and relatively small size of fluorine endow it with considerable
versatility as a bioisostere and it has found application as a substitute for lone pairs of …

The application of bioisosteres in drug discovery is a well-established design concept that
has demonstrated utility as an approach to solving a range of problems that affect candidate …

Bioisosterism is a unique approach used by medicinal chemists for the reasonable
modification of lead compounds into safer, more clinically effective, economical, and …

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 …

Incorporation of fluorine atoms or fluorine-containing functions within bioactive compounds
is considered one of the most useful approaches to address important issues relevant to …

Conspectus Allostery, or allosteric regulation, is the phenomenon in which protein functional
activity is altered by the binding of an effector at an allosteric site that is topographically …