Bioorganic and Medicinal Chemistry Letters p. 1541 - 1545 (2019)
Update date:2022-08-28
Topics:
Zhu, Mei
Dong, Biao
Zhang, Guo-Ning
Wang, Ju-Xian
Cen, Shan
Wang, Yu-Cheng
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.
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