Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors

Autor: Baker, Christopher T., Salituro, Francesco G., Court, John J., Deininger, David D., Kim, Eunice E., Li, Biquin, Novak, Perry M., Rao, Bhisetti G., Pazhanisamy, S., Schairer, Wayne C., Tung, Roger D.
Zdroj: Bioorganic & Medicinal Chemistry Letters; 1998, Vol. 8 Issue: 24 p3631-3636, 6p
Abstrakt: A combination of structure-based design and both solution, and solid-phase synthesis were utilized to derive a potent (nM) series of HIV-1 protease inhibitors bearing a structurally novel backbone. Detailed structural analysis of several inhibitors prepared in this series has suggested that rigidification of the P1/P2 region of this class of molecules may result in compounds with improved potency.
Databáze: Supplemental Index