DESIGN AND SYNTHESIS OF CINNAMIC ACID AMIDES AS CALPAIN INHIBITORS
- DESIGN AND SYNTHESIS OF CINNAMIC ACID AMIDES AS CALPAIN INHIBITORS
- 윤용돈; 윤보희; 유영재; 정서윤; 김형자; 진창배; 이용섭
- CALPAIN; STROKE; CALPAIN INHIBITOR; CINNAMIC ACID AMIDE
- Issue Date
- Drugs of the Future, Supplement A (21st International Symposium on medicinal Chemistry)
- VOL 35, 257-257
- The involvement of μ-calpain in neurological disorders, such as stroke  and Alzheimer's disease  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 . 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).
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