The newly synthetized pyridobenzoxazocynone inhibits HIV-1 reverse transcriptase activity.
We synthetized pyridobenzoxazocynone that differs in the enlarged eight-membered heterocyclic system from the basic structure of pyridobenzoxazepinones a known class of non-nucleoside HIV-1 reverse transcriptase inhibitors. Pyridobenzoxazocynone hydrochloride was found to inhibit HIV-1 reverse transcriptase activity. At concentration 0.35 microM the enzyme activity decreased by 64 +/- 14%. Higher concentrations of pyridobenzoxazocynone hydrochloride completely abolished the enzyme activity expressed as radioactivity of acid insoluble products. These results suggest that pyridobenzoxazocynones may represent a new class of HIV-1 reverse transcriptase inhibitors.
Nowak
D
D
Department of Pneumology and Allergology, Medical University of Lodz, Poland.
Glinka
R
R
Pietras
T
T
Cieslinski
M
M
Mazerant
P
P
Idowski
P
P
Leder
M
M
Sidorkiewicz
M
M
D015684:Gene Products, pol / Q000037:antagonists & inhibitors; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D006801:Humans; D015394:Molecular Structure; D010079:Oxazocines / Q000138:chemical synthesis* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology
D015684:Gene Products, pol; D010079:Oxazocines; C066027:P protein, Hepatitis B virus; D011725:Pyridines; D018894:Reverse Transcriptase Inhibitors; C113595:pyridobenzo(b,f)1,5-oxazocyn-6-one; D054303:HIV Reverse Transcriptase