Literature DB >> 16908139

Synthesis and HIV-integrase strand transfer inhibition activity of 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-ones.

Eric E Boros1, Brian A Johns, Edward P Garvey, Cecilia S Koble, Wayne H Miller.   

Abstract

An efficient synthesis of methyl 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-one-6-carboxylates (8-10 and 16) and 6-carboxamides (17-20) is described. Sub-micromolar enzyme inhibition of HIV integrase was achieved with several carboxamide analogs which were superior to their carboxylic ester congeners.

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Year:  2006        PMID： 16908139     DOI： 10.1016/j.bmcl.2006.08.007

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


  8 in total

1.  Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection.

Authors:  Tomokazu Yoshinaga; Masanori Kobayashi; Takahiro Seki; Shigeru Miki; Chiaki Wakasa-Morimoto; 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:  2014-11-03       Impact factor: 5.191

2.  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

3.  Dolutegravir (S/GSK1349572) exhibits significantly slower dissociation than raltegravir and elvitegravir from wild-type and integrase inhibitor-resistant HIV-1 integrase-DNA complexes.

Authors:  Kendra E Hightower; Ruolan Wang; Felix Deanda; Brian A Johns; Kurt Weaver; Yingnian Shen; Ginger H Tomberlin; H Luke Carter; Timothy Broderick; Scott Sigethy; Takahiro Seki; Masanori Kobayashi; Mark R Underwood
Journal:  Antimicrob Agents Chemother       Date:  2011-08-01       Impact factor: 5.191

4.  5-Methyl-3-[1-(2-pyridylmeth-yl)-1H-benzimidazol-2-ylmeth-yl]isoxazole.

Authors:  Mohamadou Lamine Doumbia; Rachid Bouhfid; El Mokhtar Essassi; Lahcen El Ammari
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-10-10

5.  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

6.  Pharmacovirological impact of an integrase inhibitor on human immunodeficiency virus type 1 cDNA species in vivo.

Authors:  Christine Goffinet; Ina Allespach; Lena Oberbremer; Pamela L Golden; Scott A Foster; Brian A Johns; Jason G Weatherhead; Steven J Novick; Karen E Chiswell; Edward P Garvey; Oliver T Keppler
Journal:  J Virol       Date:  2009-05-20       Impact factor: 5.103

7.  Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies.

Authors:  Ganesha Rai; Netra Joshi; Joo Eun Jung; Yu Liu; Lena Schultz; Adam Yasgar; Steve Perry; Giovanni Diaz; Qiangli Zhang; Victor Kenyon; Ajit Jadhav; Anton Simeonov; Eng H Lo; Klaus van Leyen; David J Maloney; Theodore R Holman
Journal:  J Med Chem       Date:  2014-05-13       Impact factor: 7.446

8.  Design, practical synthesis, and biological evaluation of novel 6-(pyrazolylmethyl)-4-quinoline-3-carboxylic acid derivatives as HIV-1 integrase inhibitors.

Authors:  Liming Hu; Song Yan; Zaigang Luo; Xiao Han; Yujie Wang; Zhanyang Wang; Chengchu Zeng
Journal:  Molecules       Date:  2012-09-06       Impact factor: 4.411
  8 in total

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