58778-51-1

Upstream product

• 3612-20-2 1-phenylmethyl-4-piperidone 
• 4783-65-7 N-benzyl-2-piperidinone 
• 402-43-7 p-trifluoromethylphenyl bromide 
• 6140-17-6 4-methylbenzotrifluoride 
• 402-51-7 4-(trifluoromethyl)phenylmagnesium bromide 

Downstream Products

• 39757-71-6 4-hydroxy-4-(α,α,α-trifluoro-p-tolyl)piperidine 
• 681482-24-6 1-benzyl-4-(4-trifluoromethyl-phenyl)-1,2,3,6-tetrahydro-pyridine 
• 1276655-88-9 1-benzyl-4-(4-(trifluoromethyl)phenyl)-piperidin-3-ol 
• 1370256-35-1 1-benzyl-4-(4-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridinium chloride 
• 58778-61-3 1-acetyl-3-{2-[4-hydroxy-4-(4-trifluoromethyl-phenyl)-piperidin-1-yl]-ethyl}-2,3-dihydro-indole 
• 58778-52-2 1,2,3,6-tetrahydro-4-(α,α,α-trifluoro-p-tolyl)-pyridine hydrochloride 

Relevant academic research and scientific papers

Focus on Human Monoamine Transporter Selectivity. New Human DAT and NET Models, Experimental Validation, and SERT Affinity Exploration

The most commonly used antidepressant drugs are the serotonin transporter inhibitors. Their effects depend strongly on the selectivity for a single monoamine transporter compared to other amine transporters or receptors, and the selectivity is roughly influenced by the spatial protein structure. Here, we provide a computational study on three human monoamine transporters, i.e., DAT, NET, and SERT. Starting from the construction of hDAT and hNET models, whose three-dimensional structure is unknown, and the prediction of the binding pose for 19 known inhibitors, 3D-QSAR models of three human transporters were built. The training set variability, which was high in structure and activity profile, was validated using a set of in-house compounds. Results concern more than one aspect. First of all, hDAT and hNET three-dimensional structures were built, validated, and compared to the hSERT one; second, the computational study highlighted the differences in binding site arrangement statistically correlated to inhibitor selectivity; third, the profiling of new inhibitors pointed out a conservation of the inhibitory activity trend between rabbit and human SERT with a difference of about 1 order of magnitude; fourth, binding and functional studies confirmed 4-(benzyloxy)-4-phenylpiperidine 20a-d and 21a-d as potent SERT inhibitors. In particular, one of the compounds (compound 20b) revealed a higher affinity for SERT than paroxetine in human platelets.

Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6- tetrahydropyridines as 5-HT2C agonists

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.

Synthesis, molecular docking and binding studies of selective serotonin transporter inhibitors

With the aim of obtaining compounds possessing high SERT selectivity, in the present work we synthesized and studied the inhibition of serotonin (SERT), dopamine (DAT) and norepinephrine (NET) transporters by docking studies and experimental binding measu

AZABENZIMIDAZOLYL COMPOUNDS

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

BENZIMIDAZOLYL COMPOUNDS AS POTENTIATORS OF MGLUR2 SUBTYPE OF GLUTAMATE RECEPTOR

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Aryl sulfonamide and sulfonyl compounds as modulators of PPAR and methods of treating metabolic disorders

Aryl sulfonamide and sulfonyl compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.

Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof

The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; p is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents an aromatic group selected from: the said aromatic groups being unsubstituted or being mono- or disubstituted by a substituent selected independently from a halogen atom; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethyl radical; Preparation process and therapeutic application.

1-Acyl-3-[2-(4-phenyl-1-piperidinyl)ethyl]indolines

This disclosure describes new substituted 1-acyl-3-[2-(4-phenyl-1-piperidinyl)ethyl]indolines which possess hypotensive activity.