Search

Your search keyword '"Glinka R"' showing total 3 results
Start Over Author "Glinka R" Topic hiv reverse transcriptase
3 results on '"Glinka R"'

1. Search for new non-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-1 RT).

Author

Brzezińska E and Glinka R

Subjects
HIV Reverse Transcriptase metabolism, Reverse Transcriptase Inhibitors chemistry, Reverse Transcriptase Inhibitors pharmacology, HIV Reverse Transcriptase antagonists & inhibitors, Reverse Transcriptase Inhibitors chemical synthesis
Abstract

The derivatives of dibenzoxazocinone, dibenzoxadiazocine, dibenzoxadiazonine, and benzodiazepine systems were synthesized as potential lead compounds for inhibitors of HIV-1 reverse transcriptase. The suggested structures were derived from analysis of the described spatial and physicochemical requirements for HIV-1 RT inhibitors. All of the evaluated compounds (apart from the oxadiazocine derivatives) showed a week inhibitory activity on recombinant HIV-1 RT from Escherichia coli.

Published
2002

2. The newly synthetized pyridobenzoxazocynone inhibits HIV-1 reverse transcriptase activity.

Author

Nowak D, Glinka R, Pietras T, Cieslinski M, Mazerant P, Idowski P, Leder M, and Sidorkiewicz M

Subjects
Gene Products, pol antagonists & inhibitors, Humans, Molecular Structure, Oxazocines pharmacology, Pyridines pharmacology, Reverse Transcriptase Inhibitors pharmacology, HIV Reverse Transcriptase antagonists & inhibitors, Oxazocines chemical synthesis, Pyridines chemical synthesis, Reverse Transcriptase Inhibitors chemical synthesis
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.

Published
1997

3. The newly synthetized pyridobenzoxazocynone inhibits HIV-1 reverse transcriptase activity

Author

Nowak, D., Glinka, R., Tadeusz Pietras, Cieslinski, M., Mazerant, P., Idowski, P., Leder, M., and Sidorkiewicz, M.

Subjects
Oxazocines, Molecular Structure, Pyridines, Gene Products, pol, Humans, Reverse Transcriptase Inhibitors, HIV Reverse Transcriptase
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.

Catalog

Books, media, physical & digital resources
See catalog results