Jones, Matthew A.; Morton, James D.; Coxon, James M.; McNabb, Stephen B.; Lee, Hannah Y.-Y.; Aitken, Steven G.; Mehrtens, Janna M.; Robertson, Lucinda J. G.; Neffe, Axel T.; Miyamoto, Shigeru; Bickerstaffe, Roy; Gately, Karl; Wood, Jacqueline M.; Abell, Andrew D. published the artcile< Synthesis, biological evaluation and molecular modeling of N-heterocyclic dipeptide aldehydes as selective calpain inhibitors>, Name: Ethyl 5-formyl-1H-pyrrole-2-carboxylate, the main research area is peptide aldehyde preparation inhibitor calpain eye lens opacification; cDNA sequence Ovis calpain 1 2 catalytic subunit.
Ten N-heterocyclic dipeptide aldehydes (4-13) have been synthesized and evaluated as inhibitors of ovine calpain 1 (o-CAPN1) and ovine calpain 2 (o-CAPN2). N-(5-formylpyrrole-2-carbonyl)-L-valylleucinal (9; IC50 values of 290 and 25 nM against o-CAPN1 and o-CAPN2, resp.) was the most potent and selective o-CAPN2 inhibitor, displaying >11-fold selectivity. The amino acid sequences of o-CAPN1 and o-CAPN2 have been determined Because of the lack of available structural information on the ovine calpains, in silico homol. models of the active site cleft of o-CAPN1 and o-CAPN2 were developed based on human calpain 1 (h-CAPN1) X-ray crystal structure (PDB code 1ZCM). These models were used to rationalize the observed SAR for compounds 4-13 and the selectivity observed for 9. The o-CAPN2 selective inhibitor 9 (CAT0059) was assayed in an in vitro ovine lens culture system and shown to successfully protect the lens from calcium-induced opacification.
Bioorganic & Medicinal Chemistry published new progress about Aldehydes Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), BIOL (Biological Study), PREP (Preparation) (dipeptides). 7126-50-3 belongs to class esters-buliding-blocks, and the molecular formula is C8H9NO3, Name: Ethyl 5-formyl-1H-pyrrole-2-carboxylate.
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