SYNTHESIS OF IRREVERSIBLE HIV-1 PROTEASE INHIBITORS CONTAINING SULFONAMIDE AND SULFONE AS AMIDE BOND ISOSTERES

Authors
CHOY N CHOI HI JUNG WH KIM CR YOON H KIM SC LEE TG KOH JS
Citation
N. Choy et al., SYNTHESIS OF IRREVERSIBLE HIV-1 PROTEASE INHIBITORS CONTAINING SULFONAMIDE AND SULFONE AS AMIDE BOND ISOSTERES, Bioorganic & medicinal chemistry letters, 7(20), 1997, pp. 2635-2638
Citations number
15
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
20
Year of publication
1997
Pages
2635 - 2638
Database
ISI
SICI code
0960-894X(1997)7:20<2635:SOIHPI>2.0.ZU;2-F
Abstract
Novel irreversible HIV-1 protease inhibitors containing sulfonamide an d sulfone as amide bond isosteres were designed, synthesized, and kine tically characterized, A representative compound 2 displayed rapid, ti me-dependent inactivation of HIV-1 protease and high potency in cell c ulture with IC50 of 6.6 nM. (C) 1997 Published by Elsevier Science Ltd .