Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists.
Journal
ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073
Informations de publication
Date de publication:
09 Jun 2022
09 Jun 2022
Historique:
received:
22
02
2022
accepted:
20
05
2022
entrez:
16
6
2022
pubmed:
17
6
2022
medline:
17
6
2022
Statut:
epublish
Résumé
Formyl peptide receptor 2 (FPR2) agonists have shown efficacy in inflammatory-driven animal disease models and have the potential to treat a range of diseases. Many reported synthetic agonists contain a phenylurea, which appears to be necessary for activity in the reported chemotypes. We set out to find isosteres for the phenylurea and focused our efforts on heteroaryl rings. The wide range of potencies with heterocyclic isosteres demonstrates how electronic effects of the heteroatom placement impact molecular recognition. Herein, we report our discovery of benzimidazole and aminophenyloxadiazole FPR2 agonists with low nanomolar activity.
Identifiants
pubmed: 35707160
doi: 10.1021/acsmedchemlett.2c00079
pmc: PMC9190041
doi:
Types de publication
Journal Article
Langues
eng
Pagination
943-948Informations de copyright
© 2022 American Chemical Society.
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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