Literature DB >> 17107799

From dihydroxypyrimidine carboxylic acids to carboxamide HIV-1 integrase inhibitors: SAR around the amide moiety.

Alessia Petrocchi1, Uwe Koch, Victor G Matassa, Barbara Pacini, Kara A Stillmock, Vincenzo Summa.   

Abstract

4,5-Dihyroxypyrimidine carboxamides, which evolved from a related series of HCV NS5b polymerase inhibitors, have been optimized to provide selective HIV integrase strand transfer inhibitors. Extensive SAR around the benzylamide moiety led to the identification of the p-fluorobenzylamide as optimal in the enzymatic assay.

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Year:  2006        PMID： 17107799     DOI： 10.1016/j.bmcl.2006.10.054

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


  8 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

3.  5,6-Dihydroxypyrimidine Scaffold to Target HIV-1 Nucleocapsid Protein.

Authors:  Savina Malancona; Mattia Mori; Paola Fezzardi; Marisabella Santoriello; Andreina Basta; Martina Nibbio; Lesia Kovalenko; Roberto Speziale; Maria Rosaria Battista; Antonella Cellucci; Nadia Gennari; Edith Monteagudo; Annalise Di Marco; Alessia Giannini; Rajhans Sharma; Manuel Pires; Eleonore Real; Maurizio Zazzi; Maria Chiara Dasso Lang; Davide De Forni; Francesco Saladini; Yves Mely; Vincenzo Summa; Steven Harper; Maurizio Botta
Journal:  ACS Med Chem Lett       Date:  2020-03-19       Impact factor: 4.345

4.  Examination of halogen substituent effects on HIV-1 integrase inhibitors derived from 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-ones and 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones.

Authors:  Xue Zhi Zhao; Kasthuraiah Maddali; B Christie Vu; Christophe Marchand; Stephen H Hughes; Yves Pommier; Terrence R Burke
Journal:  Bioorg Med Chem Lett       Date:  2009-03-28       Impact factor: 2.823

5.  Diketoacid-genre HIV-1 integrase inhibitors containing enantiomeric arylamide functionality.

Authors:  Xue Zhi Zhao; Kasthuraiah Maddali; Christophe Marchand; Yves Pommier; Terrence R Burke
Journal:  Bioorg Med Chem       Date:  2009-05-08       Impact factor: 3.641

6.  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

Review 7.  Integrase Strand Transfer Inhibitors Are Effective Anti-HIV Drugs.

Authors:  Steven J Smith; Xue Zhi Zhao; Dario Oliveira Passos; Dmitry Lyumkis; Terrence R Burke; Stephen H Hughes
Journal:  Viruses       Date:  2021-01-29       Impact factor: 5.048

8.  Discovery and Structure-Activity-Relationship Study of N-Alkyl-5-hydroxypyrimidinone Carboxamides as Novel Antitubercular Agents Targeting Decaprenylphosphoryl-β-d-ribose 2'-Oxidase.

Authors:  Sangmi Oh; Yumi Park; Curtis A Engelhart; Joshua B Wallach; Dirk Schnappinger; Kriti Arora; Michelle Manikkam; Brian Gac; Hongwu Wang; Nicholas Murgolo; David B Olsen; Michael Goodwin; Michelle Sutphin; Danielle M Weiner; Laura E Via; Helena I M Boshoff; Clifton E Barry
Journal:  J Med Chem       Date:  2018-11-05       Impact factor: 7.446
  8 in total

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