Identification and optimization of tetrahydro-2H-3-benzazepin-2-ones as squalene synthase inhibitors.

Novel squalene synthase inhibitors are disclosed. SAR and pharmacological profile of selected compounds are discussed.

Identification and characterization of the first class of potent bacterial acetyl-CoA carboxylase inhibitors with antibacterial activity.

The multisubunit acetyl-CoA carboxylase, which catalyzes the first committed step in fatty acid biosynthesis, is broadly conserved among bacteria. Its rate-limiting role in formation of fatty acids makes this enzyme an attractive target for the design of novel broad-spectrum antibacterials. However, no potent inhibitors have been discovered so far.