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Bioorg Med Chem Lett ; 98: 129595, 2024 Jan 15.
Article in English | MEDLINE | ID: mdl-38141860

ABSTRACT

Screening a library of >100,000 compounds identified the substituted tetrazole compound 1 as a selective TRPML1 agonist. Both enantiomers of compound 1 were separated and profiled in vitro and in vivo. Their selectivity, ready availability and CNS penetration should enable them to serve as the tool compounds of choice in future TRPML1 channel activation studies. SAR studies on conformationally locked macrocyclic analogs further improved the TRPML1 agonist potency while retaining the selectivity.


Subject(s)
Tetrazoles , Transient Receptor Potential Channels , Transient Receptor Potential Channels/agonists , Structure-Activity Relationship , Tetrazoles/chemistry , Tetrazoles/pharmacology
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