Inhibitory effect of 4,4′-[ethane-1,2-diylbis(sulfandiylmethanediyl)]bis(3,5-dimethyl-1H-pyrazole) and its derivatives on alpha-amylase activity

In vitro evaluation of alpha-amylase inhibition was carried out using novel representatives of sulfanyl-substituted azoles such as 4,4′-[ethane-1,2-diylbis(sulfandiylmethanediyl)]bis(3,5-dimethyl-1 H -pyrazole) ( 1 ), 4,4′-[ethane-1,2-diylbis(sulfandiylmethanediyl)]bis(3,5-dimethyl-1 H -pyrazole)·2HCl ( 2 ), 4,4′-[ethane-1,2-diylbis(sulfandiylmethanediyl)]bis(3,5-dimethyl-1,2-isoxazole) ( 3 ), and 4-(phenylsulfanylmethyl)-3,5-dimethyl-1 H -pyrazole ( 4 ). The inhibition of alpha-amylase with compound ( 1 ) was described by competitive mechanism with K i equal to 0.15 mM defined from Dixon coordinates. Results of primary screening indicated that substances ( 2 ), and ( 4 ) acted as competitive inhibitors, while ( 3 ) demonstrated characteristics of a non-competitive inhibitor.