Studies on aromatic compounds: inhibition of calpain I by biphenyl derivatives and peptide-biphenyl hybrids.
With the objective to understand structural features responsible for the biological activity, novel nonelectrophilic biphenyl derivatives and peptide-biphenyl hybrids have been synthesized and evaluated as calpain I inhibitors. The preliminary results indicate that the presence of additional aromatic rings (besides the biphenyl system) makes these compounds potent calpain inhibitors with IC50 values in the nanomolar range.
Montero
Ana
A
Instituto de Química Orgánica General, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.
Alonso
Mercedes
M
Benito
Esperanza
E
Chana
Antonio
A
Mann
Enrique
E
Navas
José M
JM
Herradón
Bernardo
B
D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D002154:Calpain / Q000037:antagonists & inhibitors*; D006801:Humans; D020128:Inhibitory Concentration 50; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D001713:Biphenyl Compounds; D009842:Oligopeptides; D011480:Protease Inhibitors; D002154:Calpain