Publication
Title
Facile access to structurally diverse antimalarial indoles using a one‐pot A³ coupling and domino cyclization approach
Author
Abstract
A multistep and diversity‐oriented synthetic route aiming at the A 3 coupling/domino cyclization of o ‐ethynyl anilines, aldehydes and s ‐amines is described. The preparation of the corresponding precursors included a series of transformations, such as haloperoxidation and Sonogashira cross‐coupling reactions, amine protection, desilylation and amine reduction. Some products of the multicomponent reaction underwent further detosylation and Suzuki coupling. The resulting library of structurally diverse compounds was evaluated against blood and liver stage malaria parasites, which revealed a promising lead with sub‐micromolar activity against intra‐erythrocytic forms of Plasmodium falciparum . The results from this hit‐to‐lead optimization are hereby reported for the first time.
Language
English
Source (journal)
ChemMedChem. - Place of publication unknown
Publication
Place of publication unknown : 2023
ISSN
1860-7179 [print]
1860-7187 [online]
DOI
10.1002/CMDC.202300264
Volume/pages
18 :17 (2023) , p. 1-5
Article Reference
e202300264
ISI
001032234000001
Pubmed ID
37392377
Medium
E-only publicatie
Full text (Publisher's DOI)
Full text (publisher's version - intranet only)
UAntwerpen
Research group
Publication type
Subject
External links
Web of Science
Record
Identifier
Creation 30.10.2023
Last edited 25.04.2024
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