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Novel pseudosymmetric inhibitors of HIV-1 protease |
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| Authors: | A. F ssler J. R sel M. Grü ther M. Tintelnot-Blomley E. Atteri G. Bold M. Lang |
| Affiliation: | Research Laboratories, Pharmaceutical Division, Ciba-Geigy Ltd., 4002 Basle, Switzerland. |
| Abstract: | Compounds containing the easily accessible Phe[CH(OH)CH2N(NH)Phe dipeptide isostere as a non-hydrolyzable replacement of the scissile amide bond in the natural substrate are potent inhibitors of HIV-1 protease. The expected symmetric binding pattern of the most potent inhibitor in this series (CGP 53280, IC50 = 9 nM) is illustrated by the X-ray analysis performed with the corresponding enzyme-inhibitor complex. |
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