57648-83-6

Upstream product

• 78069-54-2 1-(2-pyrimidinyl)piperazine hydrochloride 
• 20980-22-7 N-(2-pyridinyl)piperazine 
• 5460-29-7 2-(3-bromopropyl)isoindole-1,3-dione 
• 138274-09-6 3-(4-(pyrimidin-2-yl)piperazin-1-yl)propanenitrile 
• 206053-35-2 [3-(4-Pyrimidin-2-yl-piperazin-1-yl)-propyl]-carbamic acid tert-butyl ester 

Downstream Products

• 1227151-52-1 C₂₅H₂₉N₉O₂ 
• 1227151-51-0 C₂₅H₂₉FN₈ 
• 1227151-50-9 C₂₅H₂₉ClN₈ 
• 1227151-49-6 C₂₅H₃₀N₈ 
• 1227151-33-8 C₂₇H₂₇N₉O₂ 
• 1227151-32-7 C₂₈H₂₇N₉ 
• 1227151-31-6 C₂₇H₂₇FN₈ 
• 1227151-30-5 C₂₇H₂₇ClN₈ 
• 1227151-29-2 C₂₇H₂₇BrN₈ 
• 1227151-28-1 C₂₈H₃₀N₈ 

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.

Identification of pyridazino[4,5-b]indolizines as selective PDE4B inhibitors

Substituted pyridazino[4,5-b]indolizines were identified as potent and selective PDE4B inhibitors. We describe the structure-activity relationships generated around an HTS hit that led to a series of compounds with low nanomolar affinity for PDE4B and high selectivity over the PDE4D subtype.

5-(5,6-Dichloro-2-indolyl)-2-methoxy-2,4-pentadienamides: Novel and selective inhibitors of the vacuolar H+-ATPase of osteoclasts with bone antiresorptive activity

The vacuolar H+-ATPase (V-ATPase), located on the ruffled border of the osteoclast, is a proton pump which is responsible for secreting the massive amounts of protons that are required for the bone resorption process. With the aim to identify n

A new series of selective dopamine D4 ligands: 3-([4-arylpiperazin-1-yl]alkylamino)-2H-1,4-benzoxazines

A series of 3-([4-arylpiperaz-1-yl)alkylamino]-2H-1,4-benzoxazines were prepared and their affinities for cloned human D2, D3, and D4 dopamine receptor subtypes were measured. This led to the identification of 1a, 1f, and 1g as high affinity selective antagonists at the D4 receptor.

Synthesis and anxiolytic activity of N-substituted cyclic imides (1R*,2S*3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3-b icyclo[2.2.1]heptanedicarboxime (Tandospirone) and related compounds

A series of cyclic imides bearing a ω-(4-aryl and 4-heteroaryl-1-piperazinyl)alkyl moieties was synthesized and tested in vivo for anxiolytic activity. The in vitro binding affinities of these compounds were also examined for 5-HT(1A) receptor sites. Structure-activity relationships within these series are discussed. One of these compounds, (1R*,2S*,3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3- bicyclo[2.2.1]heptanedicarboximide (1: tandospirone), was found to be equipotent with buspirone in its anxiolytic activity and more anxio-selective than buspirone and diazepam. Tandospirone (1) is currently undergoing clinical evaluation as a selective anxiolytic agent.