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Stereoselective synthesis and discovery of novel spirooxindolopyrrolidine engrafted indandione heterocyclic hybrids as antimycobacterial agents.
Arumugam, Natarajan; Almansour, Abdulrahman I; Kumar, Raju Suresh; Siva Krishna, Vagolu; Sriram, Dharmarajan; Dege, Necmi.
Afiliação
  • Arumugam N; Department of Chemistry, College of Science, King Saud University, P.O Box 2455, Riyadh 11451, Saudi Arabia. Electronic address: anatarajan@ksu.edu.sa.
  • Almansour AI; Department of Chemistry, College of Science, King Saud University, P.O Box 2455, Riyadh 11451, Saudi Arabia.
  • Kumar RS; Department of Chemistry, College of Science, King Saud University, P.O Box 2455, Riyadh 11451, Saudi Arabia. Electronic address: sraju@ksu.edu.sa.
  • Siva Krishna V; Medicinal Chemistry and Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500078, Telangana, India.
  • Sriram D; Medicinal Chemistry and Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500078, Telangana, India.
  • Dege N; Department of Physics, Faculty of Arts and Sciences, Ondokuz Mayis University, Samsun 55139, Turkey.
Bioorg Chem ; 110: 104798, 2021 05.
Article em En | MEDLINE | ID: mdl-33735710
Novel spirooxindolopyrrolidine embedded indandione heterocyclic hybrids were obtained in excellent yields via a regio- and stereoselective one-pot three component reaction between Baylis-Hillman adduct and non-stabilized azomethine ylides. The structure of newly synthesized compounds was elucidated through 1D and 2D spectroscopic data and the stereochemistry was determined by single crystal X-ray diffraction analysis. In vitro tubercular activity against Mycobacterium tuberculosis H37Rv using MABA assay reveals that the compound bearing chlorine substituted on the oxindole ring displayed the most potent activity with MIC 0.78 µg/mL and is two-fold active than the standard drug, ethambutol (MIC 1.56 µg/mL).
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirrolidinas / Compostos de Espiro / Oxindóis / Indanos / Antibacterianos / Mycobacterium tuberculosis Idioma: En Ano de publicação: 2021 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirrolidinas / Compostos de Espiro / Oxindóis / Indanos / Antibacterianos / Mycobacterium tuberculosis Idioma: En Ano de publicação: 2021 Tipo de documento: Article