(±)-trans-2-phenyl-2,3-dihydrobenzofurans as leishmanicidal agents: Synthesis, in vitro evaluation and SAR analysis.
2-Phenyl-2,3-dihydrobenzofurans
Antileishmanial agents
Leishmania donovani
Neolignan analogues
Structure-activity relationships
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
01 Nov 2020
01 Nov 2020
Historique:
received:
12
03
2020
revised:
06
05
2020
accepted:
20
05
2020
pubmed:
4
8
2020
medline:
20
4
2021
entrez:
4
8
2020
Statut:
ppublish
Résumé
Leishmaniasis, a neglected tropical disease caused by parasites of the genus Leishmania, causes a serious burden of disease around the world, represents a threat to the life of millions of people, and therefore is a major public health problem. More effective and non-toxic new treatments are required, especially for visceral leishmaniasis, the most severe form of the disease. On the backdrop that dihydrobenzofurans have previously shown antileishmanial activity, we present here the synthesis of a set of seventy trans-2-phenyl-2,3-dihydrobenzofurans and evaluation of their in vitro activity against Leishmania donovani as well as a discussion of structure-activity relationships. Compounds 8m-o and 8r displayed the highest potency (IC
Identifiants
pubmed: 32745819
pii: S0223-5234(20)30465-7
doi: 10.1016/j.ejmech.2020.112493
pii:
doi:
Substances chimiques
Antiprotozoal Agents
0
Benzofurans
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
112493Informations de copyright
Copyright © 2020 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.