HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Thiazolobenzimidazole: biological and biochemical anti-retroviral activity of a new nonnucleoside reverse transcriptase inhibitor.

Abstract
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.
AuthorsR W Buckheit Jr, M G Hollingshead, J Germany-Decker, E L White, J B McMahon, L B Allen, L J Ross, W D Decker, L Westbrook, W M Shannon
JournalAntiviral research (Antiviral Res) Vol. 21 Issue 3 Pg. 247-65 (Jul 1993) ISSN: 0166-3542 [Print] Netherlands
PMID7692815 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • Antiviral Agents
  • Benzimidazoles
  • DNA, Single-Stranded
  • Reverse Transcriptase Inhibitors
  • Thiazoles
  • 1-(2',6'-difluorophenyl)-1H,3H-thiazolo(3,4-a)benzimidazole
  • Zidovudine
  • HIV Reverse Transcriptase
  • Didanosine
Topics
  • Antiviral Agents (pharmacology)
  • Base Sequence
  • Benzimidazoles (pharmacology)
  • Cell Line
  • DNA, Single-Stranded
  • Didanosine (pharmacology)
  • Drug Synergism
  • HIV Reverse Transcriptase
  • HIV-1 (drug effects, enzymology)
  • Humans
  • Leukemia Virus, Murine (drug effects)
  • Molecular Sequence Data
  • Molecular Structure
  • Reverse Transcriptase Inhibitors
  • Thiazoles (pharmacology)
  • Zidovudine (pharmacology)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: