Synthesis and evaluation of N-alkyl-S-[3-(piperidin-1-yl) propyl] isothioureas: High affinity and human/rat species-selective histamine H 3 receptor antagonists

S Harusawa, K Sawada, T Magata, H Yoneyama…

Index: Harusawa, Shinya; Sawada, Koichi; Magata, Takuji; Yoneyama, Hiroki; Araki, Lisa; Usami, Yoshihide; Hatano, Kouta; Yamamoto, Kouichi; Yamamoto, Daisuke; Yamatodani, Atsushi Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 23 p. 6415 - 6420

Full Text: HTML

Citation Number: 8

Abstract

Abstract S-Alkyl-N-alkylisothiourea compounds containing various cyclic amines were synthesized in the search for novel nonimidazole histamine H 3 receptor (H 3 R) antagonists. Among them, four N-alkyl S-[3-(piperidin-1-yl) propyl] isothioureas 18, 19, 22, and 23 were found to exhibit potent and selective H 3 R antagonistic activities against in vitro human H 3 R, but were inactive against in vitro human H 4 R. Furthermore, three alkyl ...