Calmodulin antagonists of improved potency and specificity for use in the study of calmodulin biochemistry.
Syntheses are described for a range of N-(omega-aminoalkyl)-5-iodo- and -5-cyanonaphthalene-1-sulphonamides. The selective activity of these compounds as inhibitors for calmodulin-dependent phosphodiesterase (EC 3.1.4.17) is compared with their activity for the calmodulin-independent but calcium-dependent enzymes protein kinase C and transglutaminase (EC 2.3.2.13). The results show a drastic improvement in the selectivity of effect for the 5-iodo-compounds compared with the widely-used drug, W7, N-(6-aminohexyl)-5-chloronaphthalene-1-sulphonamide.
D002147:Calmodulin / Q000037:antagonists & inhibitors*; D003460:Crystallization; D009281:Naphthalenes; D010726:Phosphodiesterase Inhibitors; D011493:Protein Kinase C / Q000378:metabolism; D012995:Solubility; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000494:pharmacology*; D011503:Transglutaminases / Q000378:metabolism
D002147:Calmodulin; D009281:Naphthalenes; D010726:Phosphodiesterase Inhibitors; D013449:Sulfonamides; C017967:W 7; D011503:Transglutaminases; D011493:Protein Kinase C