Benzoxazole and benzothiazole amides as novel pharmacokinetic enhancers of HIV protease inhibitors

Add time:09/24/2019    Source:sciencedirect.com

A new class of benzoxazole and benzothiazole amide derivatives exhibiting potent CYP3A4 inhibiting properties was identified. Extensive lead optimization was aimed at improving the CYP3A4 inhibitory properties as well as overall ADME profile of these amide derivatives. This led to the identification of thiazol-5-ylmethyl (2S,3R)-4-(2-(ethyl(methyl)amino)-N-isobutylbenzo[d]oxazole-6-carboxamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate (C1) as a lead candidate for this class. This compound together with structurally similar analogues demonstrated excellent ‘boosting’ properties when tested in dogs. These findings warrant further evaluation of their properties in an effort to identify valuable alternatives to Ritonavir as pharmacokinetic enhancers.

We also recommend Trading Suppliers and Manufacturers of 2-Methylthio Benzoxazole (cas 13673-62-6). Pls Click Website Link as below: cas 13673-62-6 suppliers

Prev:Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors
Next:Synthesis of substituted 2-heteroarylbenzazol-5-ol derivatives as potential ligands for estrogen receptors)