256952-65-5

Upstream product

• 1458-63-5 N-(3-chloropropyl)-piperidine 
• 99-93-4 4-Hydroxyacetophenone 
• 5472-49-1 1-(3-chloropropyl)piperidine hydrochloride 
• 110-89-4 piperidine 
• 91427-23-5 1-[4-(3-chloropropoxy)phenyl]ethanone 

Downstream Products

• 941320-54-3 3-dimethylamino-1-[4-(3-piperidin-1-yl-propoxy)-phenyl]-propan-1-one 
• 1446417-70-4 C₃₁H₄₄N₂O₃ 
• 1446417-69-1 C₃₁H₄₆N₂O₂ 
• 1029649-51-1 4-dimethylamino-1-phenyl-2-[4-(3-piperidin-1-yl-propoxy)-phenyl]-butan-2-ol 
• 1029648-95-0 N³,N³-dimethyl-N¹-phenyl-1-[4-(3-piperidin-1-yl-propoxy)-phenyl]-propane-1,3-diamine 
• 1029648-93-8 dimethyl-{4-phenyl-3-[4-(3-piperidin-1-yl-propoxy)-phenyl]-butyl}-amine 
• 1029648-98-3 dimethyl-{3-phenylsulfanyl-3-[4-(3-piperidin-1-yl-propoxy)-phenyl]-propyl}-amine 
• 1029649-54-4 1-[4-(3-piperidin-1-yl-propoxy)-phenyl]-but-3-en-1-ol 
• 1334335-19-1 C₁₈H₂₅N₃O 
• 941320-23-6 3-dimethylamino-1-[4-(3-piperidin-1-yl-propoxy)-phenyl]-propan-1-ol 
• 941320-46-3 {3-(3,4-dichloro-phenoxy)-3-[4-(3-piperidin-1-yl-propoxy)-phenyl]-propyl}-dimethyl-amine 

Relevant academic research and scientific papers

Determination of the binding mode and interacting amino-acids for dibasic H3 receptor antagonists

Due to its involvement in major CNS functions, the histamine H3 receptor (H3R) is the subject of intensive medicinal chemistry investigation, supported by the range of modern drug discovery tools, such as receptor modeling and ligand docking. Although the receptor models described to date share a majority of common traits, they display discrete alternatives in amino-acid conformation, rendering ligand binding modes quite different. Such variations impede structure-based drug design in the H3R field. In the present study, we used a combination of medicinal chemistry, receptor-guided and ligand-based methods to elucidate the binding mode of antagonists. The approaches converged towards a ligand orientation perpendicular to the membrane plane, bridging Glu206 of the transmembrane helix 5 to acidic amino acids of the extracellular loops. This consensus will help future structure-based drug design for H3R ligands.

Novel and highly potent histamine H3 receptor ligands. Part 1: Withdrawing of hERG activity

Pre-clinical investigation of some aryl-piperidinyl ether histamine H3 receptor antagonists revealed a strong hERG binding. To overcome this issue, we have developed a QSAR model specially dedicated to H3 receptor ligands. This model was designed to be di

Pyridizinone derivatives

The present invention provides compounds of formula (I*): their use as H3 inhibitors, processes for their preparation, and pharmaceutical compositions thereof.

SUBSTITUTED PHENYL PROPYL AMINES AS HISTAMINE H3 RECEPTOR AND SEROTONIN TRANSPORTER MODULATORS

Certain substituted phenyl propyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.

Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity

The synthesis and structure-activity relationships of a series of novel phenoxyphenyl diamine derivatives with affinity for both the histamine H3 receptor and the serotonin transporter is described.

Substituted acrylophenones and related mannich bases as possible spermicides and inhibitors of HIV envelope glycoprotein-CD4 interaction.

Several appropriately substituted 4-(dialkylamino-alkyl)-substituted-styryl-alkyl ketones or acetophenones were prepared and subjected to the Mannich reaction to yield compounds that would incorporate both alpha,beta-unsaturated keto groups and a substituted aminomethyl function with or without another olefinic moiety at position 4. The spermicidal activity of the prepared compounds was evaluated. Several compounds 2d, 4a and 4e were found to possess spermicidal activity at 0.005% concentration, while compounds 2a, 2c, 2f, 3a and 4b were active at 0.01% concentration. Compounds 2a, 2c, 3a, 4a and 4e also inhibited the interaction between recombinant HIV Env and CD4. Out of these, compound 2c was found to be most active.