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Tailoring selective triclosan azo-adducts: Design, synthesis, and anti-mycobacterial evaluation.
Alcaraz, Matthéo; Seboletswe, Pule; Manhas, Neha; Kremer, Laurent; Singh, Parvesh; Kumar, Vipan.
Afiliação
  • Shekhar; Department of Chemistry, Guru Nanak Dev University, Amritsar, India.
  • Alcaraz M; Centre National de la Recherche Scientifique UMR 9004, Institut de Recherche en Infectiologie de Montpellier (IRIM), Université de Montpellier, 1919 route de Mende, 34293, Montpellier, France.
  • Seboletswe P; School of Chemistry and Physics, University of KwaZulu-Natal, P/Bag X54001, Westville, Durban, South Africa.
  • Manhas N; School of Chemistry and Physics, University of KwaZulu-Natal, P/Bag X54001, Westville, Durban, South Africa.
  • Kremer L; Centre National de la Recherche Scientifique UMR 9004, Institut de Recherche en Infectiologie de Montpellier (IRIM), Université de Montpellier, 1919 route de Mende, 34293, Montpellier, France.
  • Singh P; INSERM, IRIM, 34293 Montpellier, France.
  • Kumar V; School of Chemistry and Physics, University of KwaZulu-Natal, P/Bag X54001, Westville, Durban, South Africa.
Heliyon ; 9(11): e22182, 2023 Nov.
Article em En | MEDLINE | ID: mdl-38034623
A series of triclosan azo-adducts were synthesized to investigate their structure-activity relationship against Mycobacterium tuberculosis and non-tuberculous mycobacteria. The series' most potent compound was four and sixteen times more active than triclosan and rifabutin against drug-resistant Mycobacterium abscessus, respectively, while being less cytotoxic to human macrophages than triclosan on day one. Additionally, one of the azo-adducts was twice as efficient against M. tuberculosis as triclosan and twice as effective against Mycobacterium marinum as isoniazid. Furthermore, the synthesized azo-adducts were equally effective against M. abscessus strains overexpressing InhA, suggesting that these compounds work through a distinct mechanism.
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: Heliyon Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Índia

Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: Heliyon Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Índia