51535-47-8Relevant academic research and scientific papers
Discovery of new C3aR ligands. Part 2: Amino-piperidine derivatives
Denonne, Frederic,Binet, Sophie,Burton, Maggi,Collart, Philippe,Defays, Sabine,Dipesa, Alan,Eckert, Maria,Giannaras, Alexander,Kumar, Seema,Levine, Beth,Nicolas, Jean-Marie,Pasau, Patrick,Pegurier, Cecile,Preda, Dorin,Van houtvin, Nathalie,Volosov, Andrew,Zou, Dong
, p. 3262 - 3265 (2008/02/08)
The synthesis and structure-activity relationships against the C3a receptor of a series of substituted aminopiperidine derivatives are reported. DMPK properties and functional activities of selected compounds are described. The compounds obtained are the first non-arginine ligands of C3aR.
Synthesis and Cardiovascular Activity of a New Series of Cyclohexylaralkylamine Derivatives Related to Perhexiline
Leclerc, Gerard,Decker, Nicole,Schwartz, Jean
, p. 709 - 714 (2007/10/02)
A series of 24 cyclohexylaralkylamine derivatives related to perhexilene has been synthesized and screened for cardiovascular activity.All the compounds contained an exocyclic amine which was substituted either by an alkyl, cycloalkyl, or aralkyl group.In the hope of further reducing toxicity, the synthesis of p-tolyl- and p-hydroxyphenyl derivatives 23 and 24 was undertaken.The effect of separating the cyclohexylamine moiety with respect to the aromatic nucleus has been systematically examined.The pharmacological investigations were directed to a search for compounds having an activity better than perhexiline according to the following order of criteria: (1) α-adrenolytic activity; (2) increase of coronary blood flow; (3) calcium antagonism.Several compounds were more potent and exhibited lower toxicity than perhexiline.Further detailed pharmacological investigations (tension time index and decreased cardiac work) have led to the selection of N,2-dicyclohexyl-2-phenethylamine (3) for clinical trials, which are now under way.
Solvolysis of 2-Cyclohexyl-2-phenylethyl Tosylates Substituted at the Phenyl Ring
Krstic, Vera,Muskatirovic, Milan
, p. 1637 - 1650 (2007/10/02)
The solvolysis of 2-cyclohexyl-2-phenylethyl tosylates substituted at the phenyl ring by X= p-H (1), p-NO2, p-IO2, p-CN, p-COCH3, m-Cl, m-F, p-Cl, p-Br, p-CH3, and p-OCH3 (2a-k) in ethanol, acetic acid, and formic acid has been investigated.The total rate constants kt were determined and the obtained values together with corresponding Hammett ? constants were used to calculate the rate constants kΔ (for aryl-assisted reactions) and ks (for non-assisted reactions).The acetolysis values FkΔ and ks of 2-cyclohexyl-2-phenylethyl tosylate (1) at 100 deg C are in good agreement with those formerly obtained on the basis of product analysis.
