Synthesis and HIV-1 reverse transcriptase inhibitor activity of some 2,5,6-substituted benzoxazole, benzimidazole, benzothiazole and oxazolo(4,5-b)pyridine derivatives.
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.
Akbay
Ayşegül
A
Ankara University, Faculty of Medicine, Department of Biochemistry, Ankara, Turkey.
Oren
Ilkay
I
Temiz-Arpaci
Ozlem
O
Aki-Sener
Esin
E
Yalçin
Ismail
I
D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D054306:Dideoxynucleotides; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013936:Thymidine / Q000031:analogs & derivatives* / Q000494:pharmacology; D013942:Thymine Nucleotides / Q000494:pharmacology; D015215:Zidovudine / Q000031:analogs & derivatives* / Q000494:pharmacology
D001562:Benzimidazoles; D001583:Benzoxazoles; D054306:Dideoxynucleotides; D007202:Indicators and Reagents; D011725:Pyridines; D018894:Reverse Transcriptase Inhibitors; D013844:Thiazoles; D013942:Thymine Nucleotides; C074618:5'-deoxythymidine; D015215:Zidovudine; C052873:zidovudine triphosphate; D054303:HIV Reverse Transcriptase; D013936:Thymidine