Literature DB >> 16554152

A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.

James P Guare1, John S Wai, Robert P Gomez, Neville J Anthony, Samson M Jolly, Amanda R Cortes, Joseph P Vacca, Peter J Felock, Kara A Stillmock, William A Schleif, Gregory Moyer, Lori J Gabryelski, Lixia Jin, I-Wu Chen, Daria J Hazuda, Steven D Young.   

Abstract

A series of 5-amino derivatives of 8-hydroxy[1,6]-naphthyridine-7-carboxamide exhibiting sub-micromolar potency against replication of HIV-1 in cell culture was identified. One of these analogs, compound 12, displayed excellent pharmacokinetic properties when dosed orally in rats and in monkeys. This compound was demonstrated to be efficacious against replication of simian-human immunodeficiency virus (SHIV) 89.6P in infected rhesus macaques.

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Year:  2006        PMID: 16554152     DOI: 10.1016/j.bmcl.2006.03.003

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Clinical Use of Inhibitors of HIV-1 Integration: Problems and Prospects.

Authors:  S P Korolev; Yu Yu Agapkina; M B Gottikh
Journal:  Acta Naturae       Date:  2011-07       Impact factor: 1.845

Review 2.  Authentic HIV-1 integrase inhibitors.

Authors:  Chenzhong Liao; Christophe Marchand; Terrence R Burke; Yves Pommier; Marc C Nicklaus
Journal:  Future Med Chem       Date:  2010-07       Impact factor: 3.808

Review 3.  Targeting Metalloenzymes for Therapeutic Intervention.

Authors:  Allie Y Chen; Rebecca N Adamek; Benjamin L Dick; Cy V Credille; Christine N Morrison; Seth M Cohen
Journal:  Chem Rev       Date:  2018-09-07       Impact factor: 60.622

4.  Defining the DNA substrate binding sites on HIV-1 integrase.

Authors:  James Dolan; Aiping Chen; Irene T Weber; Robert W Harrison; Jonathan Leis
Journal:  J Mol Biol       Date:  2008-11-07       Impact factor: 5.469

5.  Inhibiting the HIV integration process: past, present, and the future.

Authors:  Roberto Di Santo
Journal:  J Med Chem       Date:  2013-09-25       Impact factor: 7.446

6.  8-Hydroxy-1,6-naphthyridine-7-carboxamides as Inhibitors of Human Cytomegalovirus pUL89 Endonuclease.

Authors:  Eunkyung Jung; Ryuichi Majima; Tiffany C Edwards; Ruben Soto-Acosta; Robert J Geraghty; Zhengqiang Wang
Journal:  ChemMedChem       Date:  2022-08-10       Impact factor: 3.540

  6 in total

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