A. Nakazato, T. Kumagai, K. Ohta
Sep 3, 1999
Citations
0
Influential Citations
21
Citations
Journal
Journal of Medicinal Chemistry
Abstract
The synthesis and structure−activity relationships (SAR) of 1-alkyl-2-phenylethylamine derivatives 5−8 designed from N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]ethylamine hydrochloride (1, NE-100) are presented. The SAR between compound 1 and 1-alkyl-2-phenylethylamine derivatives suggested that the alkyl group on the 1-position carbon of 2-[4-methoxy-3-(2-phenylethyl)phenyl]ethylamine derivatives played the role of one of the propyl groups on the aminic nitrogen of compound 1. (−)-N-Propyl-1-butyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]ethylamine hydrochloride ((−)-6d, NE-537) and (−)-N-propyl-1-(3-methybutyl)-2-[4-methoxy-3-(2-phenylethoxy)phenyl]ethylamine hydrochloride ((−)-6i, NE-535), typical compounds in this series, have potent and selective σ1 affinity.