{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Rahman MS"],"funding":["University of Nebraska Medical Center","Texas Tech University","NINDS NIH HHS","National Institutes of Health"],"pagination":["128669"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8985228"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["64"],"pubmed_abstract":["Modulating peptidase neurolysin (Nln) has been identified as a potential cerebroprotective target for the development of therapeutics for ischemic stroke. Continued structure-activity relationship studies on peptidomimetic small molecule activators of Nln bearing electron-donating and electron- withdrawing functionalized phenyls are explored. Incorporation of fluorine or trifluoromethyl groups produces Nln activators with enhanced A<sub>50</sub>, while methoxy substitution produces derivatives with enhanced A<sub>max</sub>. Selected activators containing methoxy or trifluoromethyl substitution are selective for Nln over related peptidases and possess increased blood-brain barrier penetrability than initial hits."],"journal":["Bioorganic & medicinal chemistry letters"],"pubmed_title":["Structure-activity relationship studies of functionalized aromatic peptidomimetics as neurolysin activators."],"pmcid":["PMC8985228"],"funding_grant_id":["R01NS106879","R01 NS106879"],"pubmed_authors":["Kumari S","Zhang Y","Trippier PC","Abbruscato TJ","Rahman MS","Kocot J","Karamyan VT","Esfahani SH","Nozohouri S"],"additional_accession":[]},"is_claimable":false,"name":"Structure-activity relationship studies of functionalized aromatic peptidomimetics as neurolysin activators.","description":"Modulating peptidase neurolysin (Nln) has been identified as a potential cerebroprotective target for the development of therapeutics for ischemic stroke. Continued structure-activity relationship studies on peptidomimetic small molecule activators of Nln bearing electron-donating and electron- withdrawing functionalized phenyls are explored. Incorporation of fluorine or trifluoromethyl groups produces Nln activators with enhanced A<sub>50</sub>, while methoxy substitution produces derivatives with enhanced A<sub>max</sub>. Selected activators containing methoxy or trifluoromethyl substitution are selective for Nln over related peptidases and possess increased blood-brain barrier penetrability than initial hits.","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 May","modification":"2025-04-27T04:04:58.82Z","creation":"2025-04-06T19:08:39.823Z"},"accession":"S-EPMC8985228","cross_references":{"pubmed":["35292343"],"doi":["10.1016/j.bmcl.2022.128669"]}}