Synthesis and inhibitory activity on carbonic anhydrase of some new sulpiride analogues studied by means of a new method.
The pharmacological activity of several new sulpiride analogues was studied by means of a new approach, based on a potentiometric technique with a pCO2 sensor, capable of detecting carbonic anhydrase inhibition at equilibrium conditions. This procedure gives results stated as percent of inhibition of enzymatic activity (IP, inhibitory power). To prove the reliability of the proposed approach and to study structure-activity relationships, several new molecules were synthesized and tested in comparison with the two sulpiride enantiomers. A possible inhibition mechanism is discussed in terms of experimental evidence obtained from the interactions between the molecular structures of the new synthesized compounds and carbonic anhydrase.
D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011199:Potentiometry; D013329:Structure-Activity Relationship; D013469:Sulpiride / Q000031:analogs & derivatives*; D013816:Thermodynamics
D002257:Carbonic Anhydrase Inhibitors; D013469:Sulpiride