10599-17-4

Upstream product

• 92-54-6 4-phenyl-1-piperazine 
• 109-70-6 1.3-chlorobromopropane 
• 67514-07-2 1-phenyl-4-(3-hydroxypropyl)piperazine 
• 98-59-9 p-toluenesulfonyl chloride 
• 62-53-3 aniline 
• 4004-95-9 1-phenylpiperazine hydrochloride 

Downstream Products

• 101751-95-5 1-(3-diethylamino-propyl)-4-phenyl-piperazine 
• 119696-37-6 1-(4-phenyl-piperazino)-3-(4-p-tolyl-piperazino)-propane 
• 112551-52-7 1-[4-(4-chloro-phenyl)-piperazino]-3-(4-phenyl-piperazino)-propane 
• 6323-13-3 1-(4-phenyl-piperazino)-3-(4-o-tolyl-piperazino)-propane 
• 21920-26-3 6-chloro-1,1-dioxo-2-[3-(4-phenyl-piperazin-1-yl)-propyl]-1,4-dihydro-2H-1λ⁶-benzo[1,2,4]thiadiazin-3-one 
• 174519-52-9 N-<3-(4-phenylpiperazinyl-1)propyl>-1,2-ethylenediamine 
• 39577-15-6 3,4-dimethyl-7-[3-(4-phenyl-piperazin-1-yl)-propoxy]-chromen-2-one 

Relevant academic research and scientific papers

Synthesis, 5-HT(1A) and 5-HT(2A) receptor affinity of new 1-phenylpiperazinylpropyl derivatives of purine-2,6- and pyrrolidine-2,5-diones

Two series of 1-phenylpiperazinylpropyl derivatives 10, 11, 16, 17 and 19-24, structurally related to previously described 5-HT(1A) or 5-HT(2A) ligands 4 and 1, respectively, were synthesized and their binding properties were determined. Structural modifi

Discovery of phenylselenoether-hydantoin hybrids as ABCB1 efflux pump modulating agents with cytotoxic and antiproliferative actions in resistant T-lymphoma

Multidrug resistance (MDR) in cancer cells is a crucial aspect to consider for a successful cancer therapy. P-gp/ABCB1, a member of ABC transporters, is involved in the main tumour MDR mechanism, responsible for the efflux of drugs and cytotoxic substances. Herein, we describe a discovery of potent selenium-containing ABCB1 MDR efflux pump modulators with promising anticancer activity. On three groups of selenoethers comprehensive studies in terms of design, synthesis, and biological assays, including an insight into cellular mechanisms of anticancer action as well as an ADMET-screening in vitro were performed, followed by in-depth SAR analysis. Among the investigated new phenylselenoether hybrids, four compounds showed significant cytotoxic and anti-proliferative effects, in particular, in resistant cancer cells. Hydantoin derivatives (5–7) were significantly more effective than the reference inhibitor verapamil (up to 2.6-fold at a 10-fold lower concentration) modulating ABCB1-efflux pump, also possessing a good drug-drug interaction profile. The best compound (6) was further evaluated in human JURKAT T-lymphocytic cancer cells for its impact on cell proliferation rate. Mechanistically, the expression of cyclin D1, an enhancer of the cell cycle, decreases, while p53, an inhibitor of cell proliferation, was up-regulated upon the treatment with compound 6 alone or in combination with the chemotherapeutic agent doxorubicin. In summary, a new chemical space of highly active selenium-containing anticancer agents has been discovered, with a new lead compound 6 that warrants more in-depth biological evaluation and further pharmacomodulation.

Design, synthesis, and biological evaluation of structurally constrained hybrid analogues containing ropinirole moiety as a novel class of potent and selective dopamine D3 receptor ligands

Two series of hybrid analogues were designed, synthesized, and evaluated as a novel class of selective ligands for the dopamine D3 receptor. Binding affinities of target compounds were determined (using the method of radioligand binding assay). Compared to comparator agent BP897, compounds 2a and 2c were found to demonstrate a considerable binding affinity and selectivity for D3 receptor, and especially compound 2h was similarly potent and more selective D3R ligand than BP897, a positive reference. Thus, they may provide valuable information for the discovery and development of highly potent dopamine D3 receptor ligands with outstanding selectivity.

Indoline-2-ketone D3 receptor ligand and preparation method and application thereof

The invention discloses an indoline-2-ketone D3 receptor ligand, which is a compound as shown in the formula I or pharmaceutical salt thereof, wherein n=2 or 3; R represents H, 4-CH3, 2,3-diCH3, 2-CH3, 4-OCF3, 3-OCH3, 3,4-diCH3 or 4-Cl. In comparison with the prior art, the compound has a strong activity to a dopamine D3 receptor, is used in treating or preventing central nervous and metal diseases such as schizophrenia, Parkinson's disease, drug dependence and relapse, etc., can be used in neuroprotection, and is used as a tool drug for researching D3 receptor structure, function and diseases related to D3 receptor dysfunction.

Hexahydropyrazine-quinoline D3 receptor ligand and preparation method and use

The present invention discloses a hexahydropyrazino-quinoline D3 receptor ligand, which is a compound shown as formula I or a pharmaceutically acceptable salt thereof, wherein n = 2,3 or 4; R is H, 4-Cl, 2,3-diCl, 4-CH3, 2,3-diCH3, 4-OCF3, 4-OCH3, 2-OCF3, 2,6-di CH3, 3,4-di CH3, 3-CF3, 4-Cl, 3-OCH3, 2-C2H5 or 2-CH3. Compared with the prior art, the compound has strong activity to a dopamine D3 receptor, and can be used for effective treatment of Parkinson's disease, schizophrenia, drug dependence and other central nervous and mental diseases.

Design, synthesis, and biological evaluation of arylpiperazine-benzylpiperidines with dual serotonin and norepinephrine reuptake inhibitory activities

The limitations of established serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) reuptake inhibitors necessitate the development of safer and more effective therapeutic agents. Based on the structures of 4-benzylpiperidine carboxamides and trazodone, arylpiperazine-benzylpiperidines with chemical scaffolds different from those of marketed drugs were designed, synthesized, and evaluated for their neurotransmitter reuptake inhibitory activities. The majority of the synthesized compounds showed greater NE than 5-HT reuptake inhibition. The activities were even greater than those of the standard drug, venlafaxine hydrochloride were. The derivatives with a three-carbon linker showed better activities than the derivatives with a two-carbon linker. Among the newly synthesized compounds, 2d exhibited the strongest reuptake inhibition of the neurotransmitters (IC50 = 0.38 μM for NE and 1.18 μM for 5-HT). The biological activity data demonstrate that arylpiperazine-benzylpiperidines have the potential to be developed as a new class of therapeutic agents to treat neuropsychiatric and neurodegenerative disorders.

Process for preparing selected regioisomer of piperazinylalkyltriazole

The present invention refers to relates to manufacturing method for the alkyl tree which it will keep Oh it will doze piperidinyl, piperidinyl 1, 3-dipole [...] derivatives and acetylene derivatives the alkyl tree which it will keep Oh it will doze piperi

Synthesis, characterization, and anticancer studies of S and N alkyl piperazine-substituted positional isomers of 1,2,4-triazole derivatives

A series of 3-[3-[4-(substituted)-1-cyclicamine] propyl]thio-5- substituted[1,2,4]triazoles (8a-m) and 2-[3-[4-(substituted)-1-cyclicamine] propyl]-5-(substituted)-2,4-dihydro-3H[1,2,4]triazole-3-thiones (9a-h) were synthesized with good yields starting from corresponding carboxylic acids using two different methods. The cytotoxicity studies of these derivatives were studied against five different human cancer cell lines. Six compounds had shown good anticancer activity. The triazole derivatives, 9d, 8j, and 8i were most potent particularly against U937 and HL-60 cells. The cytotoxic potency of the compounds varied between the cell lines suggesting that a structural property of these compounds as possible determinant of their biological activity. Springer Science+Business Media 2013.

Synthesis of new S-alkylated-3-mercapto-1,2,4-triazole derivatives bearing cyclic amine moiety as potent anticancer agents

A series of 3-[3-[4-(Substituted)-1-cyclicamine]propyl]thio-5- substituted[1,2,4]triazoles (8a-j) were synthesized with good yields starting from corresponding carboxylic acids. The cytotoxicity studies of these derivatives were studied against five different human cancer cell lines. Three compounds had shown good anticancer activity. The triazole derivatives, 8i and 8j were most potent particularly against U937 and HL-60 cells. The cytotoxic potency of the compounds varied between the cell lines suggesting that a structural property of these compounds as possible determinants of their biological activity.

Synthesis and preliminary evaluation activity studies of novel 4-(aryl/heteroaryl-2-ylmethyl)-6-phenyl-2-[3-(4-substitutedpiperazine-1-yl) propyl]pyridazin-3(2H)-one derivatives as anticancer agents

A series of new 4-(aryl/heteroaryl-2-ylmethyl)- 6-phenyl-2-[3-(4- substituted piperazine-1-yl)propyl] pyridazin- 3(2H)-one derivatives were synthesized. The structures of the compounds were confirmed by IR, 1H NMR, and mass spectral data. All the compounds were evaluated for their cytotoxicity toward five human cancer cell lines of different origins viz; HeLa (Cervical), SKBR3 (Breast), HCT116 (Colon), A375 (Skin) & H1299 (Lung) at different concentrations and the IC50 values were determined. HCT116 and HeLa are the most sensitive against the compounds studied. One of them displayed moderate cytotoxicity against SKBR3. Majority of the compounds exhibited good to moderate activity.