دورية
Identification of MK-944a: A Second Clinical Candidate from the Hydroxylaminepentanamide Isostere Series of HIV Protease Inhibitors
| العنوان: | Identification of MK-944a: A Second Clinical Candidate from the Hydroxylaminepentanamide Isostere Series of HIV Protease Inhibitors |
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| المؤلفون: | Dorsey, B. D., McDonough, C., McDaniel, S. L., Levin, R. B., Newton, C. L., Hoffman, J. M., Darke, P. L., Zugay-Murphy, J. A., Emini, E. A., Schleif, W. A., Olsen, D. B., Stahlhut, M. W., Rutkowski, C. A., Kuo, L. C., Lin, J. H., Chen, I-W., Michelson, S. R., Holloway, M. K., Huff, J. R., Vacca, J. P. |
| المصدر: | Journal of Medicinal Chemistry; September 7, 2000, Vol. 43 Issue: 18 p3386-3399, 14p |
| مستخلص: | Recent results from human clinical trials have established the critical role of HIV protease inhibitors in the treatment of acquired immune-deficiency syndrome (AIDS). However, the emergence of viral resistance, demanding treatment protocols, and adverse side effects have exposed the urgent need for a second generation of HIV protease inhibitors. The continued exploration of our hydroxylaminepentanamide (HAPA) transition-state isostere series of HIV protease inhibitors, which initially resulted in the identification of Crixivan (indinavir sulfate, MK-639, L-735,524), has now yielded MK-944a (L-756,423). This compound is potent, is selective, and competitively inhibits HIV-1 PR with a K |
| قاعدة البيانات: | Supplemental Index |
Find this issue from the American Chemical Society | تدمد: | 00222623 15204804 |
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