Calpains are intracellular calcium dependent cysteine proteases, which are involved in regulation of various calcium-mediated biological processes. There are various isoforms of calpains which are both ubiquitous and tissue specific. Over activation of calpains have been obsereved in pathological conditions like Alzheimers, muscular dystrophy, stroke and cataracts. Therefore specific inhibitors of calpains are potential target in treatment of some of these pathological conditions. We have synthesized novel alpha-ketoamide inhibitors to investigate the effect of prime and unprime side substitutions on the potency and selectivity of calpain inhibitors across the papain class of proteases. We are currently testing these inhibitors against Calpains and Cathepsins. The synthesis and biological data will be presented at the conference.

Synthesis and biological evaluation of novel calpain inhibitors

244th National Meeting (2012)

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