Aliphatic three-and four-membered rings including cyclopropanes, cyclobutanes, oxetanes,
azetidines and bicyclo [1.1. 1] pentanes have been increasingly exploited in medicinal …

The oxetane ring is an emergent, underexplored motif in drug discovery that shows attractive
properties such as low molecular weight, high polarity, and marked three-dimensionality …

There is considerable interest in screening ultralarge chemical libraries for ligand discovery,
both empirically and computationally,,–. Efforts have focused on readily synthesizable …

Bicyclo [1.1. 1] pentanes (BCPs) are important bioisosteres of 1, 4-disubstituted arenes, tert-
butyl and acetylenic groups that can impart physicochemical benefits on drug candidates …

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 …

Carboxylic acids are an important structural feature in many drugs, but are associated with a
number of unfavorable pharmacological properties. To address this problem, carboxylic …

KAT6A and KAT6B genes are two closely related lysine acetyltransferases that transfer an
acetyl group from acetyl coenzyme A (AcCoA) to lysine residues of target histone substrates …

The hydrogen-bonding activation for 66 organocatalysts has been quantified using a 31P
NMR binding experiment with triethylphosphine oxide (TEPO). Diverse structural classes …

Oxetanes and azetidines continue to draw significant interest in medicinal chemistry, as
small, polar and non-planar motifs. Oxetanes also represent interesting surrogates for …

The N-acylsulfonamide functional group is a feature of the pharmacophore of several
biologically active molecules, including marketed drugs. Although this acidic moiety …