Category: 178928-58-0

Li, Xiang published the artcileSynthesis, Biological Evaluation, and Molecular Docking Studies of Xanthone Sulfonamides as ACAT Inhibitors, Safety of 1-(3-Cyanophenyl)piperazine, the publication is Chemical Biology & Drug Design (2015), 85(3), 394-403, database is CAplus and MEDLINE.

Three series of xanthone sulfonamides were synthesized, and their inhibitory activities against acyl-Co-A: cholesterol acyltransferase (ACAT) were evaluated. Results showed that most of the title compounds exhibited strong inhibitory activity against ACAT, and several compounds were proved to be more active than the pos. control Sandoz 58-035. Computational docking experiments indicated that the interaction between inhibitors and ACAT contained the H-bond interaction, the hydrophobic interaction, and the narrow hydrophobic cleft.

Chemical Biology & Drug Design published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Safety of 1-(3-Cyanophenyl)piperazine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Tang, Haifeng published the artcileDesign and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities, COA of Formula: C11H13N3, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(20), 6088-6092, database is CAplus and MEDLINE.

A new series of thiazole-substituted 1,1,1,3,3,3-hexafluoro-2-propanols, e.g. I, were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Key analogs caused dose-dependent decreases in food intake and body weight in obese mice. Acute treatment with these compounds also led to a drop in elevated blood glucose in a murine model of type II diabetes.

Bioorganic & Medicinal Chemistry Letters published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C19H14Cl2, COA of Formula: C11H13N3.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Chen, Peng-Jen published the artcileDesign, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine D₃ receptor ligands, Safety of 1-(3-Cyanophenyl)piperazine, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(18), 2690-2694, database is CAplus and MEDLINE.

As part of our on-going effort to explore the role of dopamine receptors in drug addiction and identify potential novel therapies for this condition, we have a identified a series of N-(4-(4-Ph piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamide D₃ ligands. Members of this class are highly selective for D₃ vs. D₂, and we have identified two compounds (13g and 13r) whose rat in vivo IV pharmacokinetic properties that indicate that they are suitable for assessment in in vivo efficacy models of substance use disorders.

Bioorganic & Medicinal Chemistry Letters published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Safety of 1-(3-Cyanophenyl)piperazine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Pettersson, Fredrik published the artcileSynthesis, pharmacological evaluation and QSAR modeling of mono-substituted 4-phenylpiperidines and 4-phenylpiperazines, Recommanded Product: 1-(3-Cyanophenyl)piperazine, the publication is European Journal of Medicinal Chemistry (2013), 241-255, database is CAplus and MEDLINE.

A series of mono-substituted 4-phenylpiperidines and -piperazines have been synthesized and their effects on the dopaminergic system tested in vivo. The structure activity relationship (SAR) revealed that the position and physicochem. character of the aromatic substituent proved to be critical for the levels of 3,4-dihydroxyphenylacetic acid (DOPAC) in the brain of freely moving rats. In order to investigate how the structural properties of these compounds affect the response, a set of tabulated and calculated physicochem. descriptors were modeled against the in vivo effects using partial least square (PLS) regression. Furthermore, the binding affinities to the dopamine D₂ (DA D₂) receptor and monoamine oxidase A (MAO A) enzyme were determined for a chosen subset and QSAR models using the same descriptors as in the in vivo model were produced to investigate the mechanisms leading to the observed DOPAC response. These models, in combination with a strong correlation between the levels of striatal DOPAC and the affinities to DA D₂ and MAO A, provide a comprehensive understanding of the biol. response for compounds in this class.

European Journal of Medicinal Chemistry published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Recommanded Product: 1-(3-Cyanophenyl)piperazine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Naito, Hiroyuki published the artcileSynthesis and antitumor activity of novel pyrimidinyl pyrazole derivatives. II. Optimization of the phenylpiperazine moiety of 1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-3-phenylpiperazinyl-1-trans-propenes, Formula: C11H13N3, the publication is Chemical & Pharmaceutical Bulletin (2002), 50(4), 453-462, database is CAplus and MEDLINE.

A series of novel 3-substituted-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propenes in order to improve the in vitro and in vivo activity of our prototype 3-[4-(3-chlorophenyl)-1-piperazinyl]-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propene (I) were synthesized and evaluated by assays of growth inhibition against several tumor cell lines in vitro and antitumor activity against some tumor models when dosed both i.p. and orally in vivo. The 3,5-difluorophenyl and 3,5-dichlorophenyl analogs of I showed significantly more potent cytotoxicity than I in vitro and potent antitumor activities without causing decrease of body temperature related to side effects.

Chemical & Pharmaceutical Bulletin published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Formula: C11H13N3.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Agai-Csongor, Eva published the artcileNovel sulfonamides having dual dopamine D2 and D3 receptor affinity show in vivo antipsychotic efficacy with beneficial cognitive and EPS profile, Recommanded Product: 1-(3-Cyanophenyl)piperazine, the publication is Bioorganic & Medicinal Chemistry Letters (2007), 17(19), 5340-5344, database is CAplus and MEDLINE.

A library of N-(heterocyclylethylcyclohexyl)arylsulfonamides such as I is prepared by automated solid-phase synthesis, with related compounds prepared by solution-phase synthesis (no data); the compounds are evaluated for their binding to the dopamine D2 and D3 receptors. I binds to the human dopamine D2 and D3 receptors with K_i values of 24 nM and 400 pM, resp.; its antipsychotic activity and cognition-enhancing activity are determined The quant. structure-activity relationship for the binding of a set of sulfonamides to dopamine D3 receptors is determined, with seven compounds evaluated on its basis for binding to dopamine D3 receptors.

Bioorganic & Medicinal Chemistry Letters published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Recommanded Product: 1-(3-Cyanophenyl)piperazine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Choi, Min Jeong published the artcileSynthesis and Biological Evaluation of Aryloxazole Derivatives as Antimitotic and Vascular-Disrupting Agents for Cancer Therapy, Category: piperazines, the publication is Journal of Medicinal Chemistry (2013), 56(22), 9008-9018, database is CAplus and MEDLINE.

Aryloxazolecarbonyl, arylthiazolecarbonyl, and arylisoxazolecarbonyl arylpiperazines and aryloxazolecarbonyl arylpiperidines such as fluorophenyloxazolecarbonyl arylpiperazines I (R = Cl, MeO) were prepared as antimitotic, antiangiogenic, and antitumor agents. Selected aryloxazolecarbonyl arylpiperazines such as I (R = Cl) inhibited angiogenesis, showed antitumor activity, and were stable to human microsomes. I (R = Cl, MeO) were tested against mice with human tumor cell (HCT-116) xenografts; I reduced the tumor size in vivo at a dose of 100 mg/kg but was toxic at a dose of 200 mg/kg.

Journal of Medicinal Chemistry published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Yadav, M. R. published the artcileDesign and synthesis of 6,7-dimethoxyquinazoline analogs as multi-targeted ligands for α₁– and AII-receptors antagonism, SDS of cas: 178928-58-0, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(13), 3959-3966, database is CAplus and MEDLINE.

Multiple-targeted ligands can have certain advantages for the management of hypertension which has multiple controls. Mols. with dual bioactivities are available in literature for treating metabolic disorders like diabetes, hypertension and hypercholesterolemia. After scrutinizing the SAR of prazosin-type α₁-blockers and AII-antagonists it was planned to develop dual α₁– and AII-antagonists. Five series of quinazoline derivatives were synthesized and evaluated as dual α₁– and AII-antagonists on rat aortic strips for the blockade of known α₁– and AII-agonist mediated contractions. Many compounds showed balanced activity on both the receptors but compound (22) was the most active derivative having higher antagonistic activity on both the receptors. In the in vivo experiments the chosen compound (22) was slightly less active than prazosin but was equipotent to losartan. These findings shed a new light on the structural requirements for both α₁– and AII-receptor antagonists.

Bioorganic & Medicinal Chemistry Letters published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C44H28ClFeN4, SDS of cas: 178928-58-0.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Povedano, Juan Manuel published the artcileA Multipronged Approach Establishes Covalent Modification of β-Tubulin as the Mode of Action of Benzamide Anti-cancer Toxins, Application of 1-(3-Cyanophenyl)piperazine, the publication is Journal of Medicinal Chemistry (2020), 63(22), 14054-14066, database is CAplus and MEDLINE.

A phenotypic high-throughput screen identified a benzamide small mol. with activity against small cell lung cancer cells. A “clickable” benzamide probe was designed that irreversibly bound a single 50 kDa cellular protein, identified by mass spectrometry as β-tubulin. Moreover, the anti-cancer potency of a series of benzamide analogs strongly correlated with probe competition, indicating that β-tubulin was the functional target. Addnl. evidence suggested that benzamides covalently modified Cys239 within the colchicine binding site. Consistent with this mechanism, benzamides impaired growth of microtubules formed with β-tubulin harboring Cys239, but not β₃ tubulin encoding Ser239. We therefore designed an aldehyde-containing analog capable of trapping Ser239 in β₃ tubulin, presumably as a hemiacetal. Using a forward genetics strategy, we identified benzamide-resistant cell lines harboring a Thr238Ala mutation in β-tubulin sufficient to induce compound resistance. The disclosed chem. probes are useful to identify other colchicine site binders, a frequent target of structurally diverse small mols.

Journal of Medicinal Chemistry published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Application of 1-(3-Cyanophenyl)piperazine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Duncton, Matthew A. J. published the artcileParallel synthesis of N-arylpiperazines using polymer-assisted reactions, Synthetic Route of 178928-58-0, the publication is Tetrahedron Letters (2006), 47(15), 2549-2552, database is CAplus.

A series of N-arylpiperazines were prepared in a parallel fashion using palladium-catalyzed cross-coupling, or nucleophilic aromatic displacement chemistries, and polymer-assisted sequestration and purification techniques as key steps.

Tetrahedron Letters published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Synthetic Route of 178928-58-0.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics