A new 5-HT3 receptor ligand. II. Structure-activity analysis of 5-HT3 receptor agonist action in the gut was written by Yamada, Megumi;Sato, Yasuo;Kobayashi, Kazuko;Konno, Fukio;Soneda, Tomoko;Watanabe, Takashi. And the article was included in Chemical & Pharmaceutical Bulletin in 1998.Category: benzoxazole This article mentions the following:
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, N 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 Probably in these 5-HT3 receptor agonists, the substituents of the benzoxazole ring influence the B-J reflex-inducing activity in rats. In the experiment, the researchers used many compounds, for example, 6-Methyl-1,3-benzoxazole-2-thiol (cas: 23417-29-0Category: benzoxazole).
6-Methyl-1,3-benzoxazole-2-thiol (cas: 23417-29-0) belongs to benzoxazole derivatives. The benzoxazole moiety is widely found in various natural compounds, which are often found to be biologically active. Due to its versatile biological properties, benzoxazole has been incorporated as an essential pharmacophore and substructure in many medicinal compounds.Category: benzoxazole
Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem