Novel Benzophenones as Non-nucleoside Reverse Transcriptase Inhibitors of HIV-1

Autor: Chan, J. H., Freeman, G. A., Tidwell, J. H., Romines, K. R., Schaller, L. T., Cowan, J. R., Gonzales, S. S., Lowell, G. S., Andrews, C. W., III, Reynolds, D. J., Clair, M. St, Hazen, R. J., Ferris, R. G., Creech, K. L., Roberts, G. B., Short, S. A., Weaver, K., Koszalka, G. W., Boone, L. R.
Zdroj: Journal of Medicinal Chemistry; February 2004, Vol. 47 Issue: 5 p1175-1182, 8p
Abstrakt: GW4511, GW4751, and GW3011 showed IC50 values ≤2 nM against wild type HIV-1 and <10 nM against 16 mutants. They were particularly potent against NNRTI-resistant viruses containing Y181C-, K103N-, and K103N-based double mutations, which account for a significant proportion of the clinical failure of the three currently marketed NNRTIs. The antiviral data together with the favorable pharmacokinetic data of GW4511 suggested that these benzophenones possess attributes of a new NNRTI drug candidate.
Databáze: Supplemental Index