Literature DB >> 24139881

IQG-607 abrogates the synthesis of mycolic acids and displays intracellular activity against Mycobacterium tuberculosis in infected macrophages.

Valnês S Rodrigues-Junior1, André A dos Santos Junior2, Anne D Villela2, Juan M Belardinelli3, Héctor R Morbidoni3, Luiz A Basso1, Maria M Campos4, Diógenes S Santos5.   

Abstract

In this work, the antitubercular activity of a pentacyano(isoniazid)ferrate(II) compound (IQG-607) was investigated using a macrophage model of Mycobacterium tuberculosis infection. Importantly, treatment of M.-tuberculosis-infected macrophages with IQG-607 significantly diminished the number of CFU compared with the untreated control group. The antitubercular activity of IQG-607 was similar to that observed for the positive control drugs isoniazid and rifampicin. Nevertheless, higher concentrations of IQG-607 produced a significantly greater reduction in bacterial load compared with the same concentrations of isoniazid. Analysis of the mechanism of action of IQG-607 revealed that the biosynthesis of mycolic acids was blocked. The promising activity of IQG-607 in infected macrophages and the experimental determination of its mechanism of action may help in further studies aimed at the development of a new antimycobacterial agent.
Copyright © 2013 Elsevier B.V. and the International Society of Chemotherapy. All rights reserved.

Entities:  

Keywords:  Drug development; IQG-607; Mycolic acid biosynthesis inhibitor; Tuberculosis

Mesh:

Substances:

Year:  2013        PMID: 24139881     DOI: 10.1016/j.ijantimicag.2013.08.021

Source DB:  PubMed          Journal:  Int J Antimicrob Agents        ISSN: 0924-8579            Impact factor:   5.283


  8 in total

1.  Revisiting Activation of and Mechanism of Resistance to Compound IQG-607 in Mycobacterium tuberculosis.

Authors:  Bruno L Abbadi; Anne D Villela; Valnês S Rodrigues-Junior; Fernanda T Subtil; Pedro F Dalberto; Ana P S Pinheiro; Diógenes S Santos; Pablo Machado; Luiz A Basso; Cristiano V Bizarro
Journal:  Antimicrob Agents Chemother       Date:  2018-01-25       Impact factor: 5.191

2.  2-(Quinolin-4-yloxy)acetamides Are Active against Drug-Susceptible and Drug-Resistant Mycobacterium tuberculosis Strains.

Authors:  Kenia Pissinate; Anne Drumond Villela; Valnês Rodrigues-Junior; Bruno Couto Giacobbo; Estêvão Silveira Grams; Bruno Lopes Abbadi; Rogério Valim Trindade; Laura Roesler Nery; Carla Denise Bonan; Davi Fernando Back; Maria Martha Campos; Luiz Augusto Basso; Diógenes Santiago Santos; Pablo Machado
Journal:  ACS Med Chem Lett       Date:  2016-01-11       Impact factor: 4.345

3.  Inhibitory activity of pentacyano(isoniazid)ferrate(II), IQG-607, against promastigotes and amastigotes forms of Leishmania braziliensis.

Authors:  Camila F Amorim; Luiza Galina; Natália B Carvalho; Nathalia D M Sperotto; Kenia Pissinate; Pablo Machado; Maria M Campos; Luiz A Basso; Valnês S Rodrigues-Junior; Edgar M Carvalho; Diógenes Santiago Santos
Journal:  PLoS One       Date:  2017-12-27       Impact factor: 3.240

4.  Construction of Mycobacterium tuberculosis cdd knockout and evaluation of invasion and growth in macrophages.

Authors:  Anne Drumond Villela; Valnês S Rodrigues-Junior; Antônio Frederico Michel Pinto; Virgínia Carla de Almeida Falcão; Zilpa Adriana Sánchez-Quitian; Paula Eichler; Cristiano Valim Bizarro; Luiz Augusto Basso; Diógenes Santiago Santos
Journal:  Mem Inst Oswaldo Cruz       Date:  2017-11       Impact factor: 2.743

5.  Evaluation of 3-Deoxy-D-Arabino-Heptulosonate 7-Phosphate Synthase (DAHPS) as a Vulnerable Target in Mycobacterium tuberculosis.

Authors:  Luiza Galina; Fernanda S M Hopf; Bruno Lopes Abbadi; Nathalia D de Moura Sperotto; Alexia M Czeczot; Mario A Duque-Villegas; Marcia Alberton Perello; Letícia Beatriz Matter; Eduardo Vieira de Souza; Tanya Parish; Pablo Machado; Luiz A Basso; Cristiano V Bizarro
Journal:  Microbiol Spectr       Date:  2022-07-14

6.  Functional, thermodynamics, structural and biological studies of in silico-identified inhibitors of Mycobacterium tuberculosis enoyl-ACP(CoA) reductase enzyme.

Authors:  Leonardo K B Martinelli; Mariane Rotta; Anne D Villela; Valnês S Rodrigues-Junior; Bruno L Abbadi; Rogério V Trindade; Guilherme O Petersen; Giuliano M Danesi; Laura R Nery; Ivani Pauli; Maria M Campos; Carla D Bonan; Osmar Norberto de Souza; Luiz A Basso; Diogenes S Santos
Journal:  Sci Rep       Date:  2017-04-24       Impact factor: 4.379

7.  Characterisation of iunH gene knockout strain from Mycobacterium tuberculosis.

Authors:  Anne Drumond Villela; Valnês da Silva Rodrigues; Antônio Frederico Michel Pinto; Priscila Lamb Wink; Zilpa Adriana Sánchez-Quitian; Guilherme Oliveira Petersen; Maria Martha Campos; Luiz Augusto Basso; Diógenes Santiago Santos
Journal:  Mem Inst Oswaldo Cruz       Date:  2017-03       Impact factor: 2.743

Review 8.  Is IQG-607 a Potential Metallodrug or Metallopro-Drug With a Defined Molecular Target in Mycobacterium tuberculosis?

Authors:  Bruno L Abbadi; Valnês da Silva Rodrigues-Junior; Adilio da Silva Dadda; Kenia Pissinate; Anne D Villela; Maria M Campos; Luiz G de França Lopes; Cristiano V Bizarro; Pablo Machado; Eduardo H S Sousa; Luiz A Basso
Journal:  Front Microbiol       Date:  2018-05-01       Impact factor: 5.640

  8 in total

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