Thiazolobenzimidazole: biological and biochemical anti-retroviral activity of a new nonnucleoside reverse transcriptase inhibitor
| Autor: | Julie Germany-Decker, Michael R. Boyd, W. Don Decker, John P. Bader, Larry J. Ross, James B. McMahon, E. Lucile White, Melinda G. Hollingshead, Lois B. Allen, Louise Westbrook, Owen S. Weislow, William M. Shannon, Robert W. Buckheit |
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| Rok vydání: | 1993 |
| Předmět: |
Molecular Sequence Data
DNA Single-Stranded Biology Antiviral Agents Virus Cell Line Virology medicine Humans Pharmacology chemistry.chemical_classification Reverse-transcriptase inhibitor Base Sequence Molecular Structure virus diseases Biological activity Drug Synergism Reverse transcriptase In vitro HIV Reverse Transcriptase Leukemia Virus Murine Didanosine Thiazoles Cell killing Enzyme chemistry Viral replication HIV-1 Reverse Transcriptase Inhibitors Benzimidazoles Zidovudine medicine.drug |
| Zdroj: | Antiviral research. 21(3) |
| ISSN: | 0166-3542 |
| Popis: | Thiazolobenzimidazole (NSC 625487) was a highly potent inhibitor of human immunodeficiency virus-induced cell killing and viral replication in a variety of human cell lines, as well as fresh human peripheral blood lymphocytes and macrophages. The compound was active against a panel of biologically diverse laboratory and clinical strains of HIV-1, including the AZT-resistant strain G910-6. However, the agent was inactive against HIV-2 and a pyridinone-resistant strain (A17) of HIV-1, a strain which is cross-resistant to several structurally diverse members of a common pharmacologic class of nonnucleoside reverse transcriptase inhibitors. The compound selectively inhibited HIV-1 reverse transcriptase but not HIV-2 reverse transcriptase. Combinations of thiazolobenzimidazole with either AZT or ddI synergistically inhibited HIV-1 induced cell killing in vitro. Thiazolobenzimidazole also inhibited the replication of the Rauscher murine leukemia retrovirus. Thus, thiazolobenzimidazole is a new active anti-HIV-1 chemotype and may represent a subclass of nonnucleoside reverse transcriptase inhibitors with an enhanced range of anti-retroviral activity. |
| Databáze: | OpenAIRE |
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