title: The newly synthetized pyridobenzoxazocynone inhibits HIV-1 reverse transcriptase activity.
abstract: 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.
authors.affiliation: Department of Pneumology and Allergology, Medical University of Lodz, Poland.
authors.forename: D
authors.initials: D
authors.lastname: Nowak
authors.forename: R
authors.initials: R
authors.lastname: Glinka
authors.forename: T
authors.initials: T
authors.lastname: Pietras
authors.forename: M
authors.initials: M
authors.lastname: Cieslinski
authors.forename: P
authors.initials: P
authors.lastname: Mazerant
authors.forename: P
authors.initials: P
authors.lastname: Idowski
authors.forename: M
authors.initials: M
authors.lastname: Leder
authors.forename: M
authors.initials: M
authors.lastname: Sidorkiewicz
mesh_terms: 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
chemical_list: 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