Synthesis and Antiviral Activity of 7-Benzyl-4-hydroxy-1, 5-naphthyridin-2 (1 H)-one HIV Integrase Inhibitors

…, M Fuji, T Fujiwara, EP Garvey, PL Golden…

Index: Boros, Eric E.; Edwards, Cynthia E.; Foster, Scott A.; Fuji, Masahiro; Fujiwara, Tamio; Garvey, Edward P.; Golden, Pamela L.; Hazen, Richard J.; Jeffrey, Jerry L.; Johns, Brian A.; Kawasuji, Takashi; Kiyama, Ryuichi; Koble, Cecilia S.; Kurose, Noriyuki; Miller, Wayne H.; Mote, Angela L.; Murai, Hitoshi; Sato, Akihiko; Thompson, James B.; Woodward, Mark C.; Yoshinaga, Tomokazu Journal of Medicinal Chemistry, 2009 , vol. 52, # 9 p. 2754 - 2761

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Citation Number: 34

Abstract

The medicinal chemistry and structure− activity relationships for a novel series of 7-benzyl-4- hydroxy-1, 5-naphthyridin-2 (1 H)-one HIV-integrase inhibitors are disclosed. Substituent effects were evaluated at the N-1, C-3, and 7-benzyl positions of the naphthyridinone ring system. Low nanomolar IC50 values were achieved in an HIV-integrase strand transfer assay with both carboxylic ester and carboxamide groups at C-3. More importantly, ...