4.7 Article

Synthesis and biological evaluation of 3,4-dihydro-1H-[1,4] oxazepino [6,5,4-hi] indol-1-ones and 4,6-dihydrooxepino [5,4,3-cd] indol-1(3H)-ones as Mycobacterium tuberculosis inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 43, Issue -, Pages -

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2021.116248

Keywords

Heterocycles; Indoles; Mycobacterium tuberculosis; Inhibitor

Funding

  1. French Ministry for Research and Innovation
  2. Fondation pour la Recherche Medicale [DEQ20150331719]
  3. Association Gregory Lemarchal and Vaincre la Mucoviscidose [RIF20180502320]

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This study focuses on the synthesis of 1,7- and 3,4-indole-fused lactones via a simple and efficient reaction sequence, with the evaluation of their activity against Mycobacterium tuberculosis showing that the oxazepino-indole structure is a new inhibitor of M. tuberculosis growth in vitro.
This study focuses on the synthesis of 1,7- and 3,4-indole-fused lactones via a simple and efficient reaction sequence. The functionalization of these oxazepino-indole and oxepino-indole tricycles is carried out by palladium catalysed C-C coupling, nucleophilic substitution or 1,3-dipolar cycloaddition. The evaluation of their activity against Mycobacterium tuberculosis shows that the oxazepino-indole structure is a new inhibitor of M. tuberculosis growth in vitro.

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