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Discovery and Synthesis of HIV Integrase Inhibitors: Development of Potent and Orally Bioavailable N-Methyl Pyrimidones

✍ Scribed by Nizi, Emanuela; Muraglia, Ester; Crescenzi, Benedetta; Ferrara, Marco; Orvieto, Federica; Pace, Paola; Pescatore, Giovanna; Poma, Marco; Rico Ferreira, Maria del Rosario; Gardelli, Cristina


Book ID
111919391
Publisher
American Chemical Society
Year
2007
Tongue
English
Weight
398 KB
Volume
50
Category
Article
ISSN
0022-2623

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A series of 2-pyrrolidinyl-N-methyl pyrimidones HIV integrase inhibitors has been explored leading to the identification of derivative 13, which showed high activity at inhibiting viral replication in cell culture, favorable pharmacokinetic profile in two preclinical species, and an attractive profi