79322-93-3

Upstream product

• 79322-92-2 3-[4-(4-chlorophenyl)-piperazin-1-yl]-propionitrile 
• 38212-33-8 4-(4-chlorophenyl) piperazine 
• 124846-92-0 2-{3-[4-(4-chlorophenyl)piperazin-1-yl]propyl}-1H-isoindole-1,3(2H)-dione 

Downstream Products

• 79323-07-2 1-{3-[4-(4-Chloro-phenyl)-piperazin-1-yl]-propyl}-4-(4-methoxy-phenyl)-piperidine-2,6-dione 
• 1240266-72-1 C₂₆H₃₃ClN₄O*ClH 
• 1360684-65-6 N-{3-[4-(4-chlorophenyl)piperazin-1-yl]propyl}-3-quinolinesulfonamide 
• 1360625-45-1 N-{3-[4-(4-chlorophenyl)piperazin-1-yl]propyl}-3-quinolinesulfonamide hydrochloride 
• 1360684-66-7 N-{3-[4-(4-chlorophenyl)piperazin-1-yl]propyl}-4-isoquinolinesulfonamide 
• 1360625-46-2 N-{3-[4-(4-chlorophenyl)piperazin-1-yl]propyl}-4-isoquinolinesulfonamide hydrochloride 
• 27105-86-8 N-{3-[4-(4-chlorophenyl)piperazin-1-yl]propyl}thiophene-2-carboxamide 

Relevant academic research and scientific papers

Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine D4 Receptor Agonists with High Subtype Selectivity

Many subtype-selective dopamine receptor ligands developed for the D2-D4 family incorporate a 1-arylpiperazine-derived primary recognition motif, which is connected to a lipophilic moiety occupying an extended binding pocket (EBP) of the receptor via an aliphatic linker of variable lengths. The evaluation of a novel group of dopamine receptor ligands now showed that highly subtype-selective ligands [up to Ki(D4.4) = 0.25 nM, D2L/D4.4 = 320, D3/D4.4 = 710 for APH199 (17)] can be obtained by choosing a relatively large and conformationally flexible 1-benzyl-1-phenylsemicarbazide substructure to fill the EBP. The novel chemotype APH199 (17) was found to act as a full agonist at the D4 receptor showing significant bias toward G protein activation over β-arrestin recruitment in comparison to quinpirole.

An interactive SAR approach to discover novel hybrid thieno probes as ligands for D2-like receptors with affinities in the subnanomolar range

A series of [(phenylpiperazinyl)alkyl]-isoindole-1,3-dione derivatives was synthesized to serve as probes for dopaminergic receptors. Among this series, compound 6a showed the highest affinity towards D4 and D3 receptors with K i values in the low nanomolar range, and D2/D4- and D2/D3-selectivity indices of 72 and 20, respectively. Optimization rounds were adopted and led to the D4-selective ligand thiophene-2-carboxamide 9a with a Ki(D4) value of 0.62 nM, and to its butyl analog, 10a, with Ki(D4) and Ki(D3) values of 0.03 and 0.26 nM, respectively. Docking experiments revealed the importance of the unique D4 residue Arg186 in manipulating the ligands' D4-subtype-receptor selectivity. Copyright

Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers

T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pain. In this study, as a part of our ongoing efforts to develop potent T-type calcium channel blockers, we designed oxazole derivatives subs