7667-37-0Relevant academic research and scientific papers
Microwave-assisted solvent-free synthesis of 3-[(4-substituted piperazin-1-yl)alkyl] imidazo[2,1-b][1,3]benzothiazol-2(3H)-ones as serotonin3 (5-HT3) receptor antagonists
Mahesh,Venkatesha Perumal,Pandi
, p. 411 - 414 (2007/10/03)
A series of novel 3-[(4-substituted piperazin-1-yl)alkyl]imidazo[2,1-b][1, 3]benzothiazol-2(3H)-ones were prepared by microwave irradiation using alumina as solid support and also by a conventional method. The compounds were characterized by spectral data and the purity was ascertained by microanalysis. The synthesized compounds were evaluated for 5-hydroxytryptamine3 antagonisms in a longitudinal muscle-myenteric plexus preparation from guinea pig ileum against the 5-hydroxytryptamine3 agonist, 2-methyl-5-hydroxytryptamine. Among the test compounds, 3-[2-(4-methylpiperazin- 1-yl)ethyl]imidazo[2,1-6][1,3]benzothiazol-2(3H)-one (3b) showed most favorable 5-hydroxytryptamine3 antagonism (pA2 6.7) in the isolated guinea pig ileum.
Synthesis and biological activity of benzotriazole derivatives structurally related to trazodone
Caliendo, G.,Carlo, R. Di,Greco, G.,Meli, R.,Novellino, E.,et al.
, p. 77 - 84 (2007/10/02)
This paper outlines the synthesis and the pharmacological screening of a series of novel 1- and 2-ethyl>benzotriazoles and 1-propoxy>benzotriazoles, which are structurally related to trazodone.Antiserotonergic, antiadrenergic and antihistaminic in vitro activity and in vivo analgesic action are described.Some of the investigated compounds show overall pharmacological profiles similar to that of the antidepressant trazodone. benzotriazole / antiserotonergic activity / antiadrenergic activity / antihistaminic activity / analgesic activity
