57479-93-3Relevant academic research and scientific papers
POTENTIAL NEUROLEPTICS OF THE ORTHOPRAMIDE SERIES; SYNTHESIS OF N-SUBSTITUTED 5-(AMINOSULFONYL)-2-METHOXYBENZAMIDES
Valenta, Vladimir,Protiva, Miroslav
, p. 2095 - 2106 (2007/10/02)
The mixed anhydride of 5-(aminosulfonyl)-2-methoxybenzoic acid (VII) and monoethyl carbonate reacted with benzylamine, 1-methylpiperazine, and 1-benzylpiperazine to give the 5-(aminosulfonyl)-2-methoxybenzamides II, IV, and V.Heating the ethyl ester X with 4-amino-1-methylpiperidine resulted in the amide III.Reaction of 5-(chlorosulfonyl)-2-methoxybenzoyl chloride (XI) with 1-benzylpiperazine afforded 5-(4-benzylpiperazinosulfonyl)-2-methoxybenzoic acid 4-benzylpiperazide (VI).Compounds II-VI are analogues of the antidopaminergic and antiemetic agent sulpiride (I) but only the benzylpiperazides V and VI showed indications of psychotropic activity of the neuroleptic type.
Synthesis and Inhibitory Activity on Carbonic Anhydrase of Some New Sulpiride Analogues Studied by Means of a New Method
Botre, Claudio,Botre, Francesco,Jommi, Giancarlo,Signorini, Roberto
, p. 1814 - 1820 (2007/10/02)
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.
