1207-00-7Relevant academic research and scientific papers
Synthesis and structure-analgesic activity relationships of a novel series of monospirocyclopiperazinium salts (MSPZ)
Lin, Song-Wen,Sun, Qi,Ge, Ze-Mei,Wang, Xin,Ye, Jia,Li, Run-Tao
, p. 940 - 943 (2011/03/21)
A series of monospirocyclopiperazinium salts were designed and synthesized to search for a peripherally-acting analgesic drug with low side effects. Extensive SAR studies revealed that a suitable NR2R3 was critical for the analgesic activity, which might be beneficial to expose the cationic nitrogen to bind to the receptor, and possibly interact with the receptor via π-π interaction. Introduction of substituting group on the N4-phenyl ring could improve the activity, and the best position was the 4-position. Compound 14n showed more potent analgesic activity (63%, 20 μM/kg, sc) and holds promise for development as a mechanically new analgesic drug.
NOVEL PIPERIDINE DERIVATIVE
-
Page/Page column 39, (2008/06/13)
The invention provides a compound of the following formula (1): wherein m, n, and p are independently an integer of 0 - 4, provided 3 ≤ m + n ≤ 8; X is nitrogen atom or a group of the formula: C-R15; Y is a substituted or unsubstituted aromatic group, etc.; R15, R1, R2, R3, R4 , R5, R6 and R7 are hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and Z is hydrogen atom, cyano group, etc., or a prodrug thereof, or a pharmaceutically acceptable salt thereof, which exhibits an action for enhancing LDL receptor expression, and is useful as a medicament for treating hyperlipidemia, atherosclerosis, etc.
