CYCLIC UREA HIV PROTEASE INHIBITORS CONTAINING ALKYNYL-TETHERED AND ALKENYL-TETHERED HETEROCYCLES IN THE P2 REGION

Authors
DAX SL COOK SC
Citation
Sl. Dax et Sc. Cook, CYCLIC UREA HIV PROTEASE INHIBITORS CONTAINING ALKYNYL-TETHERED AND ALKENYL-TETHERED HETEROCYCLES IN THE P2 REGION, Bioorganic & medicinal chemistry letters, 6(7), 1996, pp. 797-802
Citations number
4
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
7
Year of publication
1996
Pages
797 - 802
Database
ISI
SICI code
0960-894X(1996)6:7<797:CUHPIC>2.0.ZU;2-#
Abstract
A series of cyclic urea HIV protease inhibitors containing alkynyl- an d allrenyl-tethered heterocycles in the P2 region were synthesized The alkynyl compounds exhibited poor activity against the HN protease enz yme. However, reduction of the triple bond afforded trans-alkenyl deri vatives (XU348 and XU430) which displayed superb potency (sub-nanomola r K-i). Copyright (C) 1996 Elsevier Science Ltd