Synthesis and biological evaluation of new HIV-1 protease inhibitors with purine bases as P2-ligands.

ID: ALA4340543

Journal: Bioorg Med Chem Lett

Title: Synthesis and biological evaluation of new HIV-1 protease inhibitors with purine bases as P2-ligands.

Authors: Zhu M, Dong B, Zhang GN, Wang JX, Cen S, Wang YC.

Abstract: Introducing purine bases to P2-ligands might enhance the potency of Human Immunodeficiency Virus-1 (HIV-1) protease inhibitory because of the carbonyl and NH groups promoting the formation of extensive H-bonding interactions. In this work, thirty-three compounds are synthesized and evaluated, among which inhibitors 16a, 16f and 16j containing N-2-(6-substituted-9H-purin-9-yl)acetamide as the P2-ligands along with 4-methoxylphenylsulfonamide as the P2'-ligand, display potent inhibitory effect on the activity of HIV-1 protease with IC₅₀ 43 nM, 42 nM and 68 nM in vitro, respectively.

CiteXplore: 31014912

DOI: 10.1016/j.bmcl.2019.03.049

Patent ID: ┄