Structure-Activity Relationship Studies of 3- or 4-Pyridine Derivatives of DS-6930.
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:
14 Mar 2019
14 Mar 2019
Historique:
received:
20
12
2018
accepted:
25
02
2019
entrez:
21
3
2019
pubmed:
21
3
2019
medline:
21
3
2019
Statut:
epublish
Résumé
Derivatization efforts were continued to discover backups for a potent selective PPARγ modulator, DS-6930. In this Letter, the replacement of 2-pyridine ring in DS-6930 with 3- or 4-pyridyl group is reported. As the introduction of substituents on the pyridine ring did not provide potent partial agonists, modifications of benzimidazole ring were explored to discover potent intermediate agonists. 4'-Alkoxy substituted benzimidazoles failed to show potent efficacy in vivo, whereas 7'-fluoro benzimidazole
Identifiants
pubmed: 30891140
doi: 10.1021/acsmedchemlett.8b00645
pmc: PMC6421586
doi:
Types de publication
Journal Article
Langues
eng
Pagination
358-362Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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