Structure activity studies on pseudo-symmetrical HIV-1 protease inhibitors

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Abstract

Lead compound 1, obtained from a previously reported structure-assisted design approach, was optimized to 17 using a traditional medicinal chemistry approach.

A series of pseudo-symmetrical HIV-1 protease inhibitors was synthesized and evaluated for their ability to act as anti-viral agents. Compound 17 was found to be the most potent enzyme inhibitor and anti-viral agent of those prepared.

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1

Present address: Agouron Pharmaceuticals Inc. 3565 General Atomics Ct. San Diego, CA 92121

2

Department of Medicine, Hematology/Oncology Research Laboratory, New England Deaconess Hospital, Boston, MA 02215

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