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Discovery and structure-activity relationship of imidazolinylindole derivatives as kallikrein 7 inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2019 Jan 15; Vol. 29 (2), pp. 334-338. Date of Electronic Publication: 2018 Nov 08. - Publication Year :
- 2019
-
Abstract
- A series of imidazolinylindole derivatives were discovered as novel kallikrein 7 (KLK7, stratum corneum chymotryptic enzyme) inhibitors. Structure-activity relationship (SAR) studies led to the identification of potent human KLK7 inhibitors. By further modification of the benzenesulfonyl moiety to overcome species differences in inhibitory activity, potent inhibitors against both human and mouse KLK7 were identified. Furthermore, the complex structure of 25 with mouse KLK7 could explain the SAR and the cause of the species differences in inhibitory activity.<br /> (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Dose-Response Relationship, Drug
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Humans
Imidazolines chemical synthesis
Imidazolines chemistry
Indoles chemical synthesis
Indoles chemistry
Kallikreins metabolism
Mice
Molecular Structure
Structure-Activity Relationship
Drug Discovery
Enzyme Inhibitors pharmacology
Imidazolines pharmacology
Indoles pharmacology
Kallikreins antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 29
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 30522951
- Full Text :
- https://doi.org/10.1016/j.bmcl.2018.11.011