92299-77-9Relevant academic research and scientific papers
A new series of 6-chloro-2,3-dihydro-4(1H)-quinazolinone derivatives as antiemetic and gastointestinal motility enhancing agents
Baldazzi, Claudia,Barbanti, Miriam,Basaglia, Roberta,Benelli, Augusta,Bertolini, Alfio,Piani, Silvano
, p. 911 - 918 (2007/10/03)
New 6-chloro-2,3-dihydro-4(1H)-quinazolinones (24-27) have been synthesized and evaluated for gastrointestinal prokinetic and antiemetic activities in comparison with structurally related benzamides (21-22) and 6-chloro-2,3-dihydro-(1H)-1,3-benzoxazolin-4-ones (28). Their key pharmacophoric element has been defined as a 6-membered ring replacing the 'virtual ring' arising from the hydrogen bond between amidic nitrogen and methoxy group in metoclopramide (1) and structurally related benzamides (2-10). Variations of heterocycle ing groups have pointed out that a lipophilic aromatic group in position 1 plays an important role for pharmacological properties, while the steric restriction and the modification of the side-chain nucleophilicity are uneffective both for the in vitro and in vivo activity. Some of these compounds very effectively enhance gut peristaltic activity in vitro (rabbit jejunum), increase gastric emptying of a semisolid meal (in rats), and inhibit cisplatin-induced emesis (in pigeons), favourably comparing with cisapride.
Compounds with benzamidic structure active in gastro-intestinal pathologies
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, (2008/06/13)
This invention refers to compounds with benzamidic structure of general formula and their pharmacologically accepted salts. The derivatives described in this invention are active in the gastro-intestinal apparatus; in particular, they have prokinetic effects, in other words they create specific stimulation on gastro-intestinal motility, facilitating the passage of the content of the alimentary tract, and possess anti-emetic qualities, without side effects involving the central nervous system.
