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Bioorg Med Chem Lett
; 56: 128463, 2022 01 15.
Article
in English
| MEDLINE
| ID: mdl-34838652
ABSTRACT
This paper describes the structure-activity-relationships of novel fluoroalkyl substituents at the C2 position of iminothiazine dioxide beta secretase inhibitors. Key discoveries include reduced amidine basicity and its effect on Pgp, cell potency, and efficacy in various preclinical in vivo efficacy animal models. Findings from these structure-activity-relationships are discussed.