130305-58-7Relevant academic research and scientific papers
Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6- tetrahydropyridines as 5-HT2C agonists
Conway, Richard J.,Valant, Celine,Christopoulos, Arthur,Robertson, Alan D.,Capuano, Ben,Crosby, Ian T.
supporting information; experimental part, p. 2560 - 2564 (2012/05/05)
A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the 5-HT2C receptor studied to determine whether either series showed noteworthy agonist activity. Structure-activity relationships were developed from the performed receptor binding assays and functional studies, and the results of the analysis are presented herein.
FUSED HETEROCYCLIC COMPOUNDS USEFUL AS INHIBITORS OF HISTONE DEACETYLASE
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Page/Page column 172-175, (2008/06/13)
Disclosed are compounds of formula (I) that inhibit histone deacetylase (HDAC) enzymatic activity, pharmaceutical compositions comprising such compounds, as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC, wherein A, W, W1, W2, Ar2, and G are described herein.
A critical structural determinant of opioid receptor interaction with phenolic 5-phenylmorphans.
Kim, In Jong,Dersch, Christina M,Rothman, Richard B,Jacobson, Arthur E,Rice, Kenner C
, p. 4543 - 4550 (2007/10/03)
The opioid receptor binding affinities of N-methyl- and N-phenethyl-5-phenylmorphans with a meta-hydroxy substituent [3-(2-methyl-2-azabicyclo[3.3.1]non-5-yl)-phenol (1a), and 3-(2-phenethyl-2-azabicyclo[3.3.1]non-5-yl)-phenol (1b)] were compared with the
2,2-DIPHENYLBUTANAMIDE DERIVATIVES AND MEDICINES CONTAINING THE SAME
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, (2008/06/13)
2,2-Diphenylbutanamide derivatives represented by the following formula (1): [wherein A represents -(CH2)n- (n is 1 or 2) or a methine (CH) group; when A is -CH2-, B represents a methine group or a nitrogen atom, with A and B forming a single bond; when A is -(CH2)2-, B represents a nitrogen atom, with A and B forming a single bond; when A is a methine group, B represents a quaternary carbon atom, with A and B forming a double bond; each of R1 and R2, which are identical to or different from each other, represents a hydrogen atom, a lower alkyl group, or a cycloalkyl group, or R1 and R2 may form a heterocyclic ring together with the adjacent nitrogen atom; and Ar represents an optionally substituted phenyl group, bicyclic aromatic ring, monocyclic heterocyclic ring, bicyclic heterocyclic ring, or fluorene group]; or salts of the derivatives. The derivatives or salts thereof exhibit excellent μ-opioid agonist activity and analgesic activity against neuropathic pain, and are useful as medicines such as peripheral analgesic drugs and neuropathic pain relieving drugs.
Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors
Dukat, Malgorzata,Abdel-Rahman, Ashraf A.,Ismaiel, Abd M.,Ingher, Stacy,Teitler, Milt,Gyermek, Laszlo,Glennon, Richard A.
, p. 4017 - 4026 (2007/10/03)
Arylpiperazines are nonselective agents that bind at 5-HT3 serotonin receptors with moderate to high affinity, whereas 1-phenylbiguanide is a low- affinity but more selective 5-HT3 agonist. In an attempt to enhance the affinity of th
