492450-92-7Relevant academic research and scientific papers
3-Pyrroline containing arylacetamides: a novel series of remarkably selective kappa-agonists.
Mou, Qi-Yong,Chen, Jie,Zhu, You-Cheng,Zhou, De-He,Chi, Zhi-Qiang,Long, Ya-Qiu
, p. 2287 - 2290 (2007/10/03)
A series of 2-(substituted phenyl)-N-methyl-N-[(1S)-1-(substituted alkyl)-2-(1-(3-pyrrolinyl))ethyl]acetamides were synthesized and evaluated as highly selective kappa-agonists with K(i) values in low nanomolar range. 3-Pyrroline incorporated into the basic amino functionality in combination with 2-(methylthio)ethyl substituent on the carbon adjacent to the amide nitrogen remarkably enhanced the kappa-selectivity. 3,4-Dichlorophenyl derivative 1e was found the most potent and selective analgesic in this series with ED(50) value of 0.023 mg/kg.
