Abstract
In this study, the synthesis of some benzoxazoles and their analogues were described and their antiviral activities were studied together with the previously synthesized 2,5,6-trisubstituted benzoxazole, benzothiazole, benzimidazole and oxazolo(4,5-b)pyridine derivatives. The reverse transcriptase (RT) inhibitory activity of these compounds was determined using a commercial kit and assay system which utilizes the scintillation proximity assay principle. The results are concentration at which the compound inhibits RT activity by 50%). The compounds inhibited the in vitro binding of thymidine to the RT enzyme exhibiting IC50 values between 6.3 x 10(5) mumol/l-0.34 mumol/l and their activities were compared to some standard drugs such as 3'-azido-2',3'-dideoxythymidine triphosphate and dideoxythymidine triphosphate.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / pharmacology*
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Benzoxazoles / chemical synthesis*
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Benzoxazoles / pharmacology*
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Dideoxynucleotides
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HIV Reverse Transcriptase / antagonists & inhibitors*
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Indicators and Reagents
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Magnetic Resonance Spectroscopy
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Pyridines / chemical synthesis*
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Pyridines / pharmacology*
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Reverse Transcriptase Inhibitors / chemical synthesis*
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Reverse Transcriptase Inhibitors / pharmacology*
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Spectrophotometry, Infrared
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Thiazoles / chemical synthesis*
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Thiazoles / pharmacology*
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Thymidine / analogs & derivatives*
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Thymidine / pharmacology
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Thymine Nucleotides / pharmacology
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Zidovudine / analogs & derivatives*
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Zidovudine / pharmacology
Substances
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Benzimidazoles
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Benzoxazoles
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Dideoxynucleotides
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Indicators and Reagents
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Pyridines
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Reverse Transcriptase Inhibitors
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Thiazoles
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Thymine Nucleotides
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5'-deoxythymidine
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Zidovudine
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zidovudine triphosphate
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HIV Reverse Transcriptase
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Thymidine