gw-678248 and HIV-Infections

gw-678248 has been researched along with HIV-Infections* in 1 studies

Other Studies

1 other study(ies) available for gw-678248 and HIV-Infections

Article	Year
Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. Bioorganic & medicinal chemistry, 2011, Aug-01, Volume: 19, Issue:15 A novel series of benzophenone derivatives with B-ring substituted by naphthyl ring has been synthesized and evaluated as non-nucleoside HIV-1 reverse transcriptase inhibitors. Most of these compounds showed good to moderate activity against wild-type HIV-1 and mutated viruses. In particular, the analogue 10i demonstrated the most potent activity against wild-type HIV-1 with an EC₅₀ value of 4.8 nM, and with a high selectivity index up to 10347.9, it also proved to be active against the HIV-1 double mutant strain A₁₇ (K103N+Y181C) with an EC₅₀ value of 2.1 μM. In addition, the molecular modeling study was used to explore the major interactions between the potent inhibitors with the HIV-1 RT. The investigation of the structure-activity relationships may serve as an important lead for the further optimization. Topics: Anti-HIV Agents; Benzophenones; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Models, Molecular; Mutation; Reverse Transcriptase Inhibitors; Structure-Activity Relationship	2011

Article

Year

Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.

Bioorganic & medicinal chemistry, 2011, Aug-01, Volume: 19, Issue:15

A novel series of benzophenone derivatives with B-ring substituted by naphthyl ring has been synthesized and evaluated as non-nucleoside HIV-1 reverse transcriptase inhibitors. Most of these compounds showed good to moderate activity against wild-type HIV-1 and mutated viruses. In particular, the analogue 10i demonstrated the most potent activity against wild-type HIV-1 with an EC₅₀ value of 4.8 nM, and with a high selectivity index up to 10347.9, it also proved to be active against the HIV-1 double mutant strain A₁₇ (K103N+Y181C) with an EC₅₀ value of 2.1 μM. In addition, the molecular modeling study was used to explore the major interactions between the potent inhibitors with the HIV-1 RT. The investigation of the structure-activity relationships may serve as an important lead for the further optimization.

Topics: Anti-HIV Agents; Benzophenones; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Models, Molecular; Mutation; Reverse Transcriptase Inhibitors; Structure-Activity Relationship

2011