93138-61-5Relevant academic research and scientific papers
Indole, azaindole and related heterocyclic pyrrolidine derivatives
-
Page 26-27, (2008/06/13)
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity
Pyrrolidine derivatives-CCR-3 receptor antagonists
-
, (2008/06/13)
This invention relates to certain 3-aminomethylpyrrolidine derivatives of Formula (I): that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
Synthesis and pharmacological evaluation of carboxamide derivatives as selective serotoninergic 5-HT4 receptor agonists
Itoh, Katsuhiko,Kanzaki, Koji,Ikebe, Tsuguo,Kuroita, Takanobu,Tomozane, Hideo,Sonda, Shuji,Sato, Noriko,Haga, Keiichiro,Kawakita, Takeshi
, p. 329 - 341 (2007/10/03)
A number of new carboxamide derivatives were synthesized. The affinity of these compounds for the serotoninergic 5-HT4 receptor was evaluated by use of radioligand-binding techniques. The agonistic activity was evaluated as the contractile effect of the ascending colon isolated from guinea-pigs. Among these compounds, 4-amino-5-chloro-2-methoxy-N-[l-[2- [(methylsulfonyl)amino]ethly]-4piperidinylmethyl]benzamide (24) showed a high affinity for the 5-HT4 receptor (Ki = 9.6 nM). Compound 24 displayed a higher affinity for 5-HT4 receptors than the other receptors, including, 5- HT3 and dopamine D2 receptors. In addition, compound 24 was confirmed to be a potent 5-HT4 receptor agonist (ED50 = 7.0 nM). An interaction model between compound 24 and 5-HT4 receptor was proposed.
