A novel series of urea-based peptidomimetic calpain inhibitors

M Lee Sanders; Isaac O Donkor

doi:10.1016/j.bmcl.2005.12.068

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A novel series of urea-based peptidomimetic calpain inhibitors

Journal article

Peer reviewed

A novel series of urea-based peptidomimetic calpain inhibitors

M Lee Sanders and Isaac O Donkor

Bioorganic & medicinal chemistry letters, Vol.16(7), pp.1965-1968

04/01/2006

DOI: 10.1016/j.bmcl.2005.12.068

PMID: 16412635

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url

https://doi.org/10.7270/q22f7n1pView

Open Access

Abstract

A series of peptide aldehyde derivatives in which the P(2) chiral carbon has been replaced with nitrogen were synthesized as urea-based peptidomimetic inhibitors of mu-calpain. The compounds mirrored the general SAR of peptidyl aldehyde calpain inhibitors but displayed greater selectivity for mu-calpain over cathepsin B.

Molecular Mimicry

Cysteine Proteinase Inhibitors - pharmacology

Cysteine Proteinase Inhibitors - chemistry

Structure-Activity Relationship

Calpain - antagonists & inhibitors

Urea - chemistry

Urea - pharmacology

Details

Title: Subtitle: A novel series of urea-based peptidomimetic calpain inhibitors
Creators: M Lee Sanders - Department of Pharmaceutical Sciences, The University of Tennessee Health Science Center, Memphis, TN 38163, USA
Isaac O Donkor
Resource Type: Journal article
Publication Details: Bioorganic & medicinal chemistry letters, Vol.16(7), pp.1965-1968
DOI: 10.1016/j.bmcl.2005.12.068
PMID: 16412635
NLM abbreviation: Bioorg Med Chem Lett
ISSN: 0960-894X
eISSN: 1464-3405
Grant note: R21CA104982 / NCI NIH HHS
Language: English
Date published: 04/01/2006
Academic Unit: Nephrology; Internal Medicine
Record Identifier: 9984094490002771

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