BI-RG-587 is active against zidovudine-resistant human immunodeficiency virus type 1 and synergistic with zidovudine
| Autor: | R. J. Eckner, J. P. Sabo, M. Skoog, Douglas D. Richman, A. S. Rosenthal, Ting-Chao Chou, V. J. Merluzzi |
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| Rok vydání: | 1991 |
| Předmět: |
Nevirapine
Pyridines viruses T-Lymphocytes Picornaviridae Viral Plaque Assay Antiviral Agents Virus HeLa Zidovudine Cytopathogenic Effect Viral medicine Humans Pharmacology (medical) Antigens Viral Pharmacology Virus quantification biology Macrophages virus diseases Drug Resistance Microbial Drug Synergism biology.organism_classification Virology In vitro Reverse transcriptase Infectious Diseases Enzyme inhibitor HIV-2 biology.protein HIV-1 Reverse Transcriptase Inhibitors medicine.drug HeLa Cells Research Article |
| Zdroj: | Antimicrobial agents and chemotherapy. 35(2) |
| ISSN: | 0066-4804 |
| Popis: | A series of dipyridodiazepinones have been shown to be potent inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. The lead compound, BI-RG-587, had a 50% inhibitory concentration of 84 nM against HIV-1 reverse transcriptase activity. This compound reduced plaque formation of HIV-1 in HeLa cells expressing the CD4 receptor by 50% at 15 nM. BI-RG-587 at comparable concentrations inhibited the production of p24 antigen following the acute infection of CEM T-lymphoblastoid cells or primary human monocyte-derived macrophages with HIV-1. No inhibitory effects against HIV-2 or against three picornaviruses were detected. Zidovudine (3'-azido-3'-deoxythymidine [AZT])-susceptible and AZT-resistant isolates of HIV-1 were equally susceptible to BI-RG-587. AZT and BI-RG-587 exhibited synergistic inhibition of HIV-1BRU at all concentrations examined. |
| Databáze: | OpenAIRE |
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