| Abstract for PubMed entry 15537347 | |||
| Title | Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2. | |
| Authors | G.A.Freeman, C.W.Andrews Iii, A.L.Hopkins, G.S.Lowell, L.T.Schaller, J.R.Cowan, S.S.Gonzales, G.W.Koszalka, R.J.Hazen, L.R.Boone, R.G.Ferris, K.L.Creech, G.B.Roberts, S.A.Short, K.Weaver, D.J.Reynolds, J.Milton, J.Ren, D.I.Stuart, D.K.Stammers, J.H.Chan. | |
| Ref. | J Med Chem, 2004, 47, 5923-5936. | |
| PubMed id | 15537347 | |
| Abstract | ||
| 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. | ||