Abstract
A series of 1-aryl-1H,3H-thiazolo[3,4-a]benzimidazoles was synthesized starting from o-phenylenediamine, disubstituted aromatic aldehydes and 2-mercaptoacetic acid. Their antiviral activity against human immunodeficiency virus (HIV) was explored: the 1-(2',6'-dichlorophenyl) (4c), 1-(2',6'-difluorophenyl) (4i), 1-(2'-chloro,6'-fluorophenyl) (4K) and 1-(2'-chloro,5'-nitrophenyl) (4m) derivatives significantly inhibit in vitro the viral cytopathic effect in HIV-infected CEM cells. Compound 4i was selected by NCI's Review Committee for initial preclinical development studies.
MeSH terms
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Antiviral Agents / chemical synthesis*
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Antiviral Agents / chemistry
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Antiviral Agents / pharmacology
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / chemistry
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Benzimidazoles / pharmacology
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CD4-Positive T-Lymphocytes / drug effects
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CD4-Positive T-Lymphocytes / microbiology
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Chemical Phenomena
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Chemistry, Physical
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Cytopathogenic Effect, Viral / drug effects
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HIV-1 / drug effects*
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Humans
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Structure-Activity Relationship
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Thiazoles / chemical synthesis*
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Thiazoles / chemistry
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Thiazoles / pharmacology
Substances
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Antiviral Agents
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Benzimidazoles
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Thiazoles
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1-(2',6'-difluorophenyl)-1H,3H-thiazolo(3,4-a)benzimidazole