1.
Bioorg Med Chem Lett
; 80: 129048, 2023 01 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-36368496
RESUMEN
Phenotypic screening of an annotated small molecule library and initial SAR studies identified compound 2 as a robust enhancer of progranulin secretion. Detailed SAR development on conformationally restricted carbamate isosteres led to the identification of compound 60 with a 3-fold improvement in BV-2 potency and a 9-fold decrease in hERG inhibition over compound 2, substantially improving this important margin of safety relative to compound 2.