30646-50-5Relevant academic research and scientific papers
Thioxo-dihydroquinazolin-one Compounds as Novel Inhibitors of Myeloperoxidase
Li, Yang,Ganesh, Thota,Diebold, Becky A,Zhu, Yerun,McCoy, James W,Smith, Susan M. E,Sun, Aiming,Lambeth, J. David
supporting information, p. 1047 - 1052 (2015/10/20)
Myeloperoxidase (MPO) is a key antimicrobial enzyme, playing a normal role in host defense, but also contributing to inflammatory conditions including neuroinflammatory diseases such as Parkinsons and Alzheimers. We synthesized and characterized more than 50 quinazolin-4(1H)-one derivatives and showed that this class of compounds inhibits MPO with IC50 values as low as 100 nM. Representative compounds showed partially reversible inhibition that was competitive with respect to Amplex Red substrate and did not result in the accumulation of MPO Compound II. Members of this group show promise for therapeutic development for the treatment of diseases in which inflammation plays a pathogenic role.
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.
Heterocyclic compounds active in gastro-intestinal pathologies
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, (2008/06/13)
This invention refers to heterocyclic compounds of general formula STR1 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 contents of the alimentary tract, and possess anti-emetic qualities, without side effects involving the central nervous system.
Heterocyclic compounds active in gastro-intestinal pathologies
-
, (2008/06/13)
This invention refers to heterocyclic compounds 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 contents of the alimentary tract, and possess anti-emetic qualities, without side effects involving the central nervous system.
