N-(4-Fluorobenzyl)-3-hydroxy-9,9-dimethyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrazino[1,2-a]pyrimidine-2-carboxamides a novel class of potent HIV-1 integrase inhibitors |
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| Authors: | Alessia Petrocchi Philip Jones Michael Rowley Fabrizio Fiore Vincenzo Summa |
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| Affiliation: | Departments of Medicinal Chemistry and Drug Metabolism IRBM-MRL, Via Pontina, Km 30.600, 00040 Pomezia (RM), Italy |
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| Abstract: | A novel class of tetrahydro-pyrazinopyrimidine-2-carboxamides have been identified as HIV-1 integrase inhibitors. Optimization of the initial lead culminated in the discovery of a series of compounds with high potency on the enzyme and an antiviral cell-based activity equivalent to that showed by Raltegravir, the first in class HIV-1 integrase inhibitor. |
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