Literature DB >> 19217284

1,3,4-Oxadiazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 2: SAR of the C5 position.

Brian A Johns1, Jason G Weatherhead, Scott H Allen, James B Thompson, Edward P Garvey, Scott A Foster, Jerry L Jeffrey, Wayne H Miller.   

Abstract

The use of a 1,3,4-oxadiazole in combination with an 8-hydroxy-1,6-naphthyridine ring system has been shown to deliver potent enzyme and antiviral activity through inhibition of viral DNA integration. This report presents a detailed structure-activity investigation of the C5 position resulting in low nM potency for several analogs with an excellent therapeutic index.

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Year:  2009        PMID： 19217284     DOI： 10.1016/j.bmcl.2009.01.089

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


  8 in total

Review 1.  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

2.  6,7-Dihydroxy-1-oxoisoindoline-4-sulfonamide-containing HIV-1 integrase inhibitors.

Authors:  Xue Zhi Zhao; Kasthuraiah Maddali; Steven J Smith; Mathieu Métifiot; Barry C Johnson; Christophe Marchand; Stephen H Hughes; Yves Pommier; Terrence R Burke
Journal:  Bioorg Med Chem Lett       Date:  2012-10-27       Impact factor: 2.823

3.  Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140.

Authors:  Chris P Miller; Maysoun Shomali; C Richard Lyttle; Louis St L O'Dea; Hillary Herendeen; Kyla Gallacher; Dottie Paquin; Dennis R Compton; Bishwabhusan Sahoo; Sean A Kerrigan; Matthew S Burge; Michael Nickels; Jennifer L Green; John A Katzenellenbogen; Alexei Tchesnokov; Gary Hattersley
Journal:  ACS Med Chem Lett       Date:  2010-12-02       Impact factor: 4.345

4.  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

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.  Copper-Catalyzed One-Pot Synthesis of 2,5-Disubstituted 1,3,4-Oxadiazoles from Arylacetic Acids and Hydrazides via Dual Oxidation.

Authors:  Chinnari Lekkala; Varaprasad Bodala; Kumari Yettula; Bharat Kumar Karasala; Rajitha Lakshmi Podugu; Siddaiah Vidavalur
Journal:  ACS Omega       Date:  2022-07-27

Review 7.  Antimicrobial Activity of 1,3,4-Oxadiazole Derivatives.

Authors:  Teresa Glomb; Piotr Świątek
Journal:  Int J Mol Sci       Date:  2021-06-29       Impact factor: 5.923

Review 8.  Synthetic approaches and pharmacological activity of 1,3,4-oxadiazoles: a review of the literature from 2000-2012.

Authors:  Cledualdo Soares de Oliveira; Bruno Freitas Lira; José Maria Barbosa-Filho; Jorge Gonçalo Fernandez Lorenzo; Petrônio Filgueiras de Athayde-Filho
Journal:  Molecules       Date:  2012-08-27       Impact factor: 4.411
  8 in total

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