Tricyclic ureas: a new class of HIV-1 protease inhibitors |
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Authors: | W Han JC Pelletier CN Hodge |
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Affiliation: | Department of Chemical and Physical Sciences, DuPont Pharmaceuticals Company, Wilmington, Delaware 19880-0500, USA. |
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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. |
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