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Development of 2-pyrrolidinyl-N-methyl pyrimidones as potent and orally bioavailable HIV integrase inhibitors

✍ Scribed by Marco Ferrara; Fabrizio Fiore; Vincenzo Summa; Cristina Gardelli

Book ID: 104004649
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 524 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.07.042

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✦ Synopsis

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 profile against a panel of HIV-integrase mutants.

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