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Design and synthesis of 4-Aminoquinoline-isoindoline-dione-isoniazid triads as potential anti-mycobacterials.
Rani, Anu; Johansen, Matt D; Roquet-Banères, Françoise; Kremer, Laurent; Awolade, Paul; Ebenezer, Oluwakemi; Singh, Parvesh; Kumar, Vipan.
Afiliação
  • Rani A; Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India.
  • Johansen MD; Institut de Recherche en Infectiologie (IRIM) de Montpellier, CNRS, UMR 9004 Université de Montpellier, France.
  • Roquet-Banères F; Institut de Recherche en Infectiologie (IRIM) de Montpellier, CNRS, UMR 9004 Université de Montpellier, France.
  • Kremer L; Institut de Recherche en Infectiologie (IRIM) de Montpellier, CNRS, UMR 9004 Université de Montpellier, France; INSERM, IRIM, 34293 Montpellier, France.
  • Awolade P; School of Chemistry and Physics, University of KwaZulu-Natal, P/Bag X54001, Westville, Durban, South Africa.
  • Ebenezer O; School of Chemistry and Physics, University of KwaZulu-Natal, P/Bag X54001, Westville, Durban, South Africa.
  • Singh P; School of Chemistry and Physics, University of KwaZulu-Natal, P/Bag X54001, Westville, Durban, South Africa.
  • Sumanjit; Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India.
  • Kumar V; Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India. Electronic address: vipan_org@yahoo.com.
Bioorg Med Chem Lett ; 30(22): 127576, 2020 11 15.
Article em En | MEDLINE | ID: mdl-32980514
A series of 4-aminoquinoline-isoindoline-dione-isoniazid triads were synthesized and assessed for their anti-mycobacterial activities and cytotoxicity. Most of the synthesized compounds exhibited promising activities against the mc26230 strain of M. tuberculosis with MIC in the range of 5.1-11.9 µM and were non-cytotoxic against Vero cells. The conjugates lacking either isoniazid or quinoline core in their structural framework failed to inhibit the growth of M. tuberculosis; thus, further strengthening the proposed design of triads in the present study.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Aminoquinolinas / Indóis / Isoniazida / Mycobacterium tuberculosis / Antituberculosos Idioma: En Ano de publicação: 2020 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Aminoquinolinas / Indóis / Isoniazida / Mycobacterium tuberculosis / Antituberculosos Idioma: En Ano de publicação: 2020 Tipo de documento: Article