39223-94-4Relevant academic research and scientific papers
A new 5-HT3 receptor ligand. II. Structure-activity analysis of 5-HT3 receptor agonist action in the gut
Yamada, Megumi,Sato, Yasuo,Kobayashi, Kazuko,Konno, Fukio,Soneda, Tomoko,Watanabe, Takashi
, p. 445 - 451 (2007/10/03)
Several modified 2-piperazinyl benzoxazole derivatives, which exhibit an agonistic effect on gastrointestinal motility, were synthesized and their effects on the contraction of guinea-pig ileum were examined. The quaternary piperazinyl benzoxazole structure has a restricted conformation and stereostructure compared to those of the other 5-HT3 receptor agonists, serotonin and meta-chlorophenylbiguanide. The mutual positions of the aromatic ring, nitrogen atom and terminal amine are considered to form the pharmacophore of the 5-HT3 receptor agonist in the gut. In the serotonin- evoked reflex bradycardia [Bezold-Jarisch (B-J) reflex] inhibition test using rats the B-J reflex-inducing ratio was different for each synthesized compound. These results suggest that, in these 5-HT3 receptor agonists, the substituents of the benzoxazole ring influence the B-J reflex-inducing activity in rats.
2-Phenoxy, -phenylthio-, and -phenyl-amino-benzoxazoles having an isothiocyano substituent
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, (2008/06/13)
Isothiocyano substituted 2-phenoxy, 2-phenylthio and 2-phenylamino-benzoxazoles have anthelmintic activity in warm-blooded animals. Included are compounds of the formula SPC1 In which one of R2 and R5 is isothiocyano and the other is
