THE NEWLY SYNTHESIZED PYRIDOBENZOXAZOCYNONE INHIBITS HIV-1 REVERSE-TRANSCRIPTASE ACTIVITY

We synthetized pyridobenzoxazocynone that differs in the enlarged eigh t-membered heterocyclic system from the basic structure of pyridobenzo xazepinones a known class of non-nucleoside HIV-1 reverse transcriptas e inhibitors. Pyridobenzoxazocynone hydrochloride was found to inhibit HIV-1 reverse transcriptase activity. At concentration 0.35 mu M the enzyme activity decreased by 64 +/- 14%. Higher concentrations of pyri dobenzoxazocynone hydrochloride completely abolished the enzyme activi ty expressed as radioactivity of acid insoluble products. These result s suggest that pyridobenzoxazocynones may represent a new class of HIV -1 reverse transcriptase inhibitors.