AI Article Synopsis
- A new group of compounds called imidazolinylindole derivatives have been found to effectively inhibit kallikrein 7 (KLK7), an enzyme involved in skin function.
- Research into the structure-activity relationship (SAR) revealed several strong inhibitors for human KLK7.
- Modifications were made to enhance the efficacy of these inhibitors for both human and mouse KLK7, and a detailed structure of one compound helped clarify the differences in how these inhibitors work across species.
Article 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.
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| http://dx.doi.org/10.1016/j.bmcl.2018.11.011 | DOI Listing |
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