Discovery of 3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one derivatives as a new class of ROCK inhibitors for the treatment of glaucoma.
Glaucoma
IOP-lowering effect
ROCK inhibitors
Structure–activity relationship
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
01 08 2021
01 08 2021
Historique:
received:
05
02
2021
revised:
16
05
2021
accepted:
20
05
2021
pubmed:
28
5
2021
medline:
6
1
2022
entrez:
27
5
2021
Statut:
ppublish
Résumé
The Rho-associated protein kinases (ROCKs) are associated with the pathology of glaucoma and discovery of ROCK inhibitors has attracted much attention in recent years. Herein, we report a series of 3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one derivatives as a new class of ROCK inhibitors. Structure-activity relationship studies led to the discovery of compound 12b, which showed potent activities against ROCK I and ROCK Ⅱ with IC
Identifiants
pubmed: 34044123
pii: S0960-894X(21)00364-4
doi: 10.1016/j.bmcl.2021.128138
pii:
doi:
Substances chimiques
Oxazepines
0
ROCK1 protein, human
EC 2.7.11.1
ROCK2 protein, human
EC 2.7.11.1
rho-Associated Kinases
EC 2.7.11.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
128138Informations de copyright
Copyright © 2021 Elsevier Ltd. All rights reserved.