vrx-480773 and acetanilide

vrx-480773 has been researched along with acetanilide* in 1 studies

Other Studies

1 other study(ies) available for vrx-480773 and acetanilide

Article	Year
Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors. Bioorganic & medicinal chemistry, 2015, Aug-01, Volume: 23, Issue:15 A novel series of etravirine-VRX-480773 hybrids were designed using structure-guided molecular hybridization strategy and fusing the pharmacophore templates of etravirine and VRX-480773. The anti-HIV-1 activity and cytotoxicity was evaluated in MT-4 cell cultures. The most active hybrid compound in this series, N-(2-chlorophenyl)-2-((4-(4-cyano-2,6-dimethylphenoxy)pyrimidin-2-yl)thio)acetamide 3d (EC50=0.24 , SI>1225), was more potent than delavirdine (EC50=0.66 μM, SI>67) in the anti-HIV-1 in vitro cellular assay. Studies of structure-activity relationships established a correlation between anti-HIV activity and the substitution pattern of the acetanilide group. Topics: Acetanilides; Anti-HIV Agents; Cell Line; Chemistry Techniques, Synthetic; Drug Discovery; Drug Evaluation, Preclinical; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Dynamics Simulation; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Triazoles	2015

Article

Year

Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.

Bioorganic & medicinal chemistry, 2015, Aug-01, Volume: 23, Issue:15

A novel series of etravirine-VRX-480773 hybrids were designed using structure-guided molecular hybridization strategy and fusing the pharmacophore templates of etravirine and VRX-480773. The anti-HIV-1 activity and cytotoxicity was evaluated in MT-4 cell cultures. The most active hybrid compound in this series, N-(2-chlorophenyl)-2-((4-(4-cyano-2,6-dimethylphenoxy)pyrimidin-2-yl)thio)acetamide 3d (EC50=0.24 , SI>1225), was more potent than delavirdine (EC50=0.66 μM, SI>67) in the anti-HIV-1 in vitro cellular assay. Studies of structure-activity relationships established a correlation between anti-HIV activity and the substitution pattern of the acetanilide group.

Topics: Acetanilides; Anti-HIV Agents; Cell Line; Chemistry Techniques, Synthetic; Drug Discovery; Drug Evaluation, Preclinical; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Dynamics Simulation; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Triazoles

2015