Related Experiment Videos
Tricyclic ureas: a new class of HIV-1 protease inhibitors
W Han1, J C Pelletier, C N Hodge
1Department of Chemical and Physical Sciences, DuPont Pharmaceuticals Company, Wilmington, Delaware 19880-0500, USA.
Bioorganic & Medicinal Chemistry Letters
|February 6, 1999
Abstract:
A new class of tricyclic ureas containing a conformationally constrained proline was designed with the aid of molecular modeling. Efficient stereoselective intermolecular pinacol coupling represented the highlight of the synthesis. These rigid cyclic ureas are active towards HIV-1 protease, with 9 being the most potent compound (Ki = 9 nM) despite interacting with only three side chain binding pockets of HIV protease.