The identification of potent and selective orexin-2 receptor (OX 2 R) antagonists is described
based on the modification of N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline analogue …

The structure–activity relationships of xanthene carboxamide derivatives on the CCR1
receptor binding affinity and the functional antagonist activity were described. Previously, we …

DNA gyrase and topoisomerase IV are well-validated pharmacological targets, and quinolone
antibacterial drugs are marketed as their representative inhibitors. However, in recent …

A new class of 1β-methylcarbapenems bearing a doubly quaternarized 1,4-diazabicyclooctane
(DABCO) substituted dithiocarbamate moiety at the C-2 side chain was prepared, and …

The CC chemokines may play an important role in the pathogenesis of chronic inflammatory
diseases including rheumatoid arthritis, and their effects are thought to be mediated through …

We describe design, syntheses and structure–activity relationships of a novel class of 4,6-disubstituted
quinazoline glucokinase activators. Prototype quinazoline leads (4 and 5) were …

UDP-3-O-acyl-N-acetylglucosamine deacetylase (LpxC) is a zinc metalloenzyme that catalyzes
the first committed step in the biosynthesis of Lipid A, an essential component of the cell …

In searching for a novel CCR3 receptor antagonist, we designed a library that included a
variety of carboxamide derivatives based on the structure of our potent antagonists for human …

Design, syntheses, and structure–activity relationships of a novel class of 2-{3-oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole
NPY Y5 receptor antagonists are …

A novel series of (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamides was
designed and synthesized based on the structure and biological profiles of an active …