4-Thiazolidinones were synthesized and evaluated for their ability to inhibit the bacterial
enzyme MurB. Selected 4-thiazolidinones displayed activity against the enzyme in vitro. This …

During the course of our research efforts to develop a potent and selective γ-secretase
inhibitor for the treatment of Alzheimer's disease, we investigated a series of carboxamide-…

Nocathiacins are cyclic thiazolyl peptides with inhibitory activity against gram-positive bacteria.
BMS-249524 (nocathiacin I), identified from screening a library of compounds against a …

… Author links open overlay panel Joanne J Bronson , Kenneth L DenBleyker , Paul J Falk ,
Robert A Mate , Hsu-Tso Ho , Michael J Pucci , Lawrence B Snyder … Reagents and conditions …

The acyclic nucleotide analogue (S)-l-[3-hydroxy-2-(phosphonylmethoxy) propyl] cytosine (2,
HPMPC) was prepared on a multigram scale in 18% overall yield starting from (R)-2, 3-0-…

A series of 9-(phosphonoalkyl) purines, which are analogues of 9-[2-(phosphonomethoxy)
ethyl] purines (guanine, PMEG, 1; adenine, PMEA, 2), were synthesized. The analogues were …

Recent mouse knockout studies identified adapter protein-2 associated kinase 1 (AAK1) as
a viable target for treating neuropathic pain. Potent small-molecule inhibitors of AAK1 have …

Detailed metabolic characterization of 8, an earlier lead pyrazinone-based corticotropin-releasing
factor-1 (CRF 1 ) receptor antagonist, revealed that this compound formed significant …

The synthesis and antibacterial activity of a series of nocathiacin I derivatives (4–20) containing
polar water solubilizing groups is described. Thiol-Michael adducts containing acidic …

Recent mouse knockout studies identified adapter protein-2-associated kinase 1 (AAK1) as
a viable target for treating neuropathic pain. BMS-986176/LX-9211 (4), as a highly selective, …