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First Insight Into Structure-Activity Relationships of Selective Meprin β Inhibitors

First Insight Into Structure-Activity Relationships of Selective Meprin β Inhibitors

Daniel Ramsbeck, Antje Hamann, Dagmar Schlenzig, Stephan Schilling, Mirko Buchholz

Bioorg Med Chem Lett. 2017 Jun 1;27(11):2428-2431.

PMID: 28408220

Abstract:

The astacin proteases meprin α and β are emerging drug targets for treatment of disorders such as kidney failure, fibrosis or inflammatory bowel disease. However, there are only few inhibitors of both proteases reported to date. Starting from NNGH as lead structure, a detailed elaboration of the structure-activity relationship of meprin β inhibitors was performed, leading to compounds with activities in the lower nanomolar range. Considering the preference of meprin β for acidic residues in the P1' position, the compounds were optimized. Acidic modifications induced potent inhibition and >100-fold selectivity over other structurally related metalloproteases such as MMP-2 or ADAM10.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP161314176-B	NNGH		161314-17-6	Price

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