Literature DB >> 17194584

A potent and orally active HIV-1 integrase inhibitor.

Melissa S Egbertson1, H Marie Moritz, Jeffrey Y Melamed, Wei Han, Debra S Perlow, Michelle S Kuo, Mark Embrey, Joseph P Vacca, Matthew M Zrada, Amanda R Cortes, Audrey Wallace, Yvonne Leonard, Daria J Hazuda, Michael D Miller, Peter J Felock, Kara A Stillmock, Marc V Witmer, William Schleif, Lori J Gabryelski, Gregory Moyer, Joan D Ellis, Lixia Jin, Wei Xu, Matthew P Braun, Kellem Kassahun, Nancy N Tsou, Steven D Young.   

Abstract

A 1,6-naphthyridine inhibitor of HIV-1 integrase has been discovered with excellent inhibitory activity in cells, good pharmacokinetics, and an excellent ability to inhibit virus with mutant enzyme.

Entities:  

Mesh：

Substances：

Year:  2006        PMID： 17194584     DOI： 10.1016/j.bmcl.2006.11.080

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


  10 in total

1.  In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.

Authors:  Masanori Kobayashi; Tomokazu Yoshinaga; Takahiro Seki; Chiaki Wakasa-Morimoto; Kevin W Brown; Robert Ferris; Scott A Foster; Richard J Hazen; Shigeru Miki; Akemi Suyama-Kagitani; Shinobu Kawauchi-Miki; Teruhiko Taishi; Takashi Kawasuji; Brian A Johns; Mark R Underwood; Edward P Garvey; Akihiko Sato; Tamio Fujiwara
Journal:  Antimicrob Agents Chemother       Date:  2010-11-29       Impact factor: 5.191

2.  Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance.

Authors:  Stephen Hare; Ann M Vos; Reginald F Clayton; Jan W Thuring; Maxwell D Cummings; Peter Cherepanov
Journal:  Proc Natl Acad Sci U S A       Date:  2010-10-28       Impact factor: 11.205

Review 3.  Multiple ways of targeting APOBEC3-virion infectivity factor interactions for anti-HIV-1 drug development.

Authors:  Jessica L Smith; Wei Bu; Ryan C Burdick; Vinay K Pathak
Journal:  Trends Pharmacol Sci       Date:  2009-12       Impact factor: 14.819

4.  The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.

Authors:  Edward P Garvey; Brian A Johns; Margaret J Gartland; Scott A Foster; Wayne H Miller; Robert G Ferris; Richard J Hazen; Mark R Underwood; Eric E Boros; James B Thompson; Jason G Weatherhead; Cecilia S Koble; Scott H Allen; Lee T Schaller; Ronald G Sherrill; Tomokazu Yoshinaga; Masanori Kobayashi; Chiaki Wakasa-Morimoto; Shigeru Miki; Koichiro Nakahara; Takeshi Noshi; Akihiko Sato; Tamio Fujiwara
Journal:  Antimicrob Agents Chemother       Date:  2007-12-26       Impact factor: 5.191

5.  Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.

Authors:  Gregg S Jones; Fang Yu; Ameneh Zeynalzadegan; Joseph Hesselgesser; Xiaowu Chen; James Chen; Haolun Jin; Choung U Kim; Matthew Wright; Romas Geleziunas; Manuel Tsiang
Journal:  Antimicrob Agents Chemother       Date:  2008-12-22       Impact factor: 5.191

6.  Synthesis and anti-HSV-1 evaluation of new 3H-benzo[b]pyrazolo[3,4-h]-1,6-naphthyridines and 3H-pyrido[2,3-b]pyrazolo[3,4-h]-1,6-naphthyridines.

Authors:  Alice Mr Bernardino; Alexandre R Azevedo; Luiz Cs Pinheiro; Júlio C Borges; Izabel Cp Paixão; Milene Mesquita; Thiago Ml Souza; Maurício S Dos Santos
Journal:  Org Med Chem Lett       Date:  2012-02-01

7.  HIV integrase variability and genetic barrier in antiretroviral naïve and experienced patients.

Authors:  Antonio Piralla; Stefania Paolucci; Roberto Gulminetti; Giuditta Comolli; Fausto Baldanti
Journal:  Virol J       Date:  2011-03-31       Impact factor: 4.099

8.  An expedient synthesis, acetylcholinesterase inhibitory activity, and molecular modeling study of highly functionalized hexahydro-1,6-naphthyridines.

Authors:  Abdulrahman I Almansour; Raju Suresh Kumar; Natarajan Arumugam; Alireza Basiri; Yalda Kia; Mohamed Ashraf Ali
Journal:  Biomed Res Int       Date:  2015-01-29       Impact factor: 3.411

9.  Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent In Vitro Antileishmanial Activity: Initial SAR and Assessment of In Vivo Activity.

Authors:  Michael G Thomas; Manu De Rycker; Richard J Wall; Daniel Spinks; Ola Epemolu; Sujatha Manthri; Suzanne Norval; Maria Osuna-Cabello; Stephen Patterson; Jennifer Riley; Frederick R C Simeons; Laste Stojanovski; John Thomas; Stephen Thompson; Claire Naylor; Jose M Fiandor; Paul G Wyatt; Maria Marco; Susan Wyllie; Kevin D Read; Timothy J Miles; Ian H Gilbert
Journal:  J Med Chem       Date:  2020-08-13       Impact factor: 7.446

10.  Natural variation of HIV-1 group M integrase: implications for a new class of antiretroviral inhibitors.

Authors:  Soo-Yon Rhee; Tommy F Liu; Mark Kiuchi; Rafael Zioni; Robert J Gifford; Susan P Holmes; Robert W Shafer
Journal:  Retrovirology       Date:  2008-08-07       Impact factor: 4.602
  10 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.