Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.

Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.

HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) are part of the combination therapy currently used to treat HIV infection. The features of a new NNRTI drug for HIV treatment must include selective potent activity against both wild-type virus as well as against mutant virus that have be...

Full description

Bibliographic Details
Main Authors: Freeman, G, Andrews, C, Hopkins, A, Lowell, G, Schaller, LT, Cowan, JR, Gonzales, S, Koszalka, G, Hazen, R, Boone, L, Ferris, R, Creech, K, Roberts, G, Short, SA, Weaver, K, Reynolds, D, Milton, J, Ren, J, Stuart, D, Stammers, D, Chan, J
Format: Journal article
Language:English
Published: 2004
Description
Summary:HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) are part of the combination therapy currently used to treat HIV infection. The features of a new NNRTI drug for HIV treatment must include selective potent activity against both wild-type virus as well as against mutant virus that have been selected by use of current antiretroviral treatment regimens. Based on analogy with known HIV-1 NNRTI inhibitors and modeling studies utilizing the X-ray crystal structure of inhibitors bound in the HIV-1 RT, a series of substituted 2-quinolones was synthesized and evaluated as HIV-1 inhibitors.

Similar Items