Logo image
Sign in
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 article   Open access   Peer reviewed

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

Bastien Champciaux, Clément Raynaud, Albertus Viljoen, Loïc Chene, Jérôme Thibonnet, Stéphane Vincent, Laurent Kremer and Emilie Thiery
Bioorganic and Medicinal Chemistry Letters, Vol.43
08/2021

Abstract

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 palladocatalyzed CC 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.
url
Find in HALView
url
https://doi.org/10.1016/j.bmc.2021.116248View
Published (Version of record) Open

Metrics

1 Record Views

Details

Logo image