1.
Arch Pharm (Weinheim)
; 345(6): 431-43, 2012 Jun.
Article
in English
| MEDLINE
| ID: mdl-22415744
ABSTRACT
Novel, potent non-imidazole histamine H(3) receptor antagonists were prepared. Detailed structure-activity studies revealed that N-(4-trifluoromethylbenzyl)-N-[4-(7-phenoxyheptylpiperazin-1-yl)butyl]guanidine (pA(2) = 8.49 ± 0.05), 1h, and N-(4-nitrobenzyl)-N-[4-(7-phenoxyheptylpiperazin-1-yl)butyl]guanidine (pA(2) = 8.43 ± 0.05), 1l, exhibit high affinity for the H(3) histamine receptor. The most potent antagonists in this series, 1e, 1h, and 1l, were also in vitro tested as H(1) receptor antagonists, showing weak H(1) -antagonistic activity with pA(2) = 6.70 ± 0.09, pA(2) = 6.46 ± 0.09, and pA(2) = 6.65 ± 0.11, respectively.