Download MendeleyA New Class of HIV-1 Protease Inhibitors Containing a Tertiary Alcohol in the Transition-State Mimicking Scaffold.
Ekegren, J.K., Unge, T., Safa, M.Z., Wallberg, H., Samuelsson, B., Hallberg, A.(2005) J Med Chem 48: 8098
- PubMed: 16335934
- DOI: https://doi.org/10.1021/jm050790t
- Primary Citation of Related Structures:
2BQV - PubMed Abstract:
Novel HIV-1 protease inhibitors encompassing a tertiary alcohol as part of the transition-state mimicking unit have been synthesized. Variation of the P1'-P3' residues and alteration of the tertiary alcohol absolute stereochemistry afforded 10 inhibitors. High potencies for the compounds with (S)-configuration at the carbon carrying the tertiary hydroxyl group were achieved with Ki values down to 2.4 nM. X-ray crystallographic data for a representative compound in complex with HIV-1 protease are presented.
Organizational Affiliation:
Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry, BMC, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden.
