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- W1991570653 abstract "Novel prolylcarboxypeptidase (PrCP) inhibitors with nanomolar IC50 values were prepared by replacing the previously described dichlorobenzimidazole-substituted pyrrolidine amides with a variety of substituted benzylamine amides. In contrast to prior series, the compounds demonstrated minimal inhibition shift in whole serum and minimal recognition by P-glycoprotein (P-gp) efflux transporters. The compounds were also cell permeable and demonstrated in vivo brain exposure. The in vivo effect of compound (S)-6e on weight loss in an established diet-induced obesity (eDIO) mouse model was studied." @default.
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- W1991570653 date "2012-01-01" @default.
- W1991570653 modified "2023-10-11" @default.
- W1991570653 title "The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors" @default.
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- W1991570653 doi "https://doi.org/10.1016/j.bmcl.2011.10.060" @default.
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