DESIGN AND SYNTHESIS OF CINNAMIC ACID AMIDES AS CALPAIN INHIBITORS

Title
DESIGN AND SYNTHESIS OF CINNAMIC ACID AMIDES AS CALPAIN INHIBITORS
Authors
윤용돈윤보희유영재정서윤김형자진창배이용섭
Keywords
CALPAIN; STROKE; CALPAIN INHIBITOR; CINNAMIC ACID AMIDE
Issue Date
2010-09
Publisher
Drugs of the Future, Supplement A (21st International Symposium on medicinal Chemistry)
Citation
VOL 35, 257-257
Abstract
The involvement of μ-calpain in neurological disorders, such as stroke [1] and Alzheimer's disease [2] has attracted considerable interest in the use of calpain inhibitors as therapeutic agents. In the present study, a series of cinnamoyl acid amides were designed and synthesized as acyclic analogs of calpain inhibitory chromone carboxamides [3]. Cinnamoyt acid amides possessing an alkyl chain at the α-position showed approximately 10-fold more potent μ-calpain inhibitory activities than an unsubstituted derivative (IC50 = 6.07 μM). Among synthesized, then-butyl-substituted cinnamoyl acid amide showed the most potent μ-calpain inhibitory activity (IC50 = 0.13 μM) comparableto those of the chromone carboxamides, indicating that the Cinnamoyl skeleton can be regarded as an acyclic variant of the chromone ring. This work was supported by the Basic Science Research Program through the National Research Foundation of korea(NRF) funded by MEST(2010-0016080).
URI
http://pubs.kist.re.kr/handle/201004/38745
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KIST Publication > Conference Paper
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