Month: November 2022

Bodner, Ruth A. published the artcilePharmacological promotion of inclusion formation: a therapeutic approach for Huntington’s and Parkinson’s diseases, Recommanded Product: (4-Chlorophenyl)(4-(8-nitroquinolin-5-yl)piperazin-1-yl)methanone, the publication is Proceedings of the National Academy of Sciences of the United States of America (2006), 103(11), 4246-4251, database is CAplus and MEDLINE.

Misfolded proteins accumulate in many neurodegenerative diseases, including huntingtin in Huntington’s disease and α-synuclein in Parkinson’s disease. The disease-causing proteins can take various conformations and are prone to aggregate and form larger cytoplasmic or nuclear inclusions. One approach to the development of therapeutic intervention for these diseases has been to identify chem. compounds that reduce the size or number of inclusions. We have, however, identified a compound that promotes inclusion formation in cellular models of both Huntington’s disease and Parkinson’s disease. Of particular interest, this compound prevents huntingtin-mediated proteasome dysfunction and reduces α-synuclein-mediated toxicity. These results demonstrate that compounds that increase inclusion formation may actually lessen cellular pathol. in both Huntington’s and Parkinson’s diseases, suggesting a therapeutic approach for neurodegenerative diseases caused by protein misfolding.

Proceedings of the National Academy of Sciences of the United States of America published new progress about 115687-05-3. 115687-05-3 belongs to piperazines, auxiliary class Epigenetics,Sirtuin, name is (4-Chlorophenyl)(4-(8-nitroquinolin-5-yl)piperazin-1-yl)methanone, and the molecular formula is C20H17ClN4O3, Recommanded Product: (4-Chlorophenyl)(4-(8-nitroquinolin-5-yl)piperazin-1-yl)methanone.

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

Tsou, Hwei-Ru published the artcile4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as Potent and Selective Inhibitors of the Cyclin-Dependent Kinase 4 (CDK4), Product Details of C10H16N4, the publication is Journal of Medicinal Chemistry (2008), 51(12), 3507-3525, database is CAplus and MEDLINE.

The cyclin-dependent kinases (CDKs), as complexes with their resp. partners, the cyclins, are critical regulators of cell cycle progression. Because aberrant regulations of CDK4/cyclin D1 lead to uncontrolled cell proliferation, a hallmark of cancer, small-mol. inhibitors of CDK4/cyclin D1 are attractive as prospective antitumor agents. The series of 4-(phenylaminomethylene)isoquinoline-1,3(2H,4H)-dione derivatives reported here represents a novel class of potent inhibitors that selectively inhibit CDK4 over CDK2 and CDK1 activities. In the headpiece of the 4-(phenylaminomethylene)isoquinoline-1,3(2H,4H)-dione, a basic amine substitutent is required on the aniline ring for the CDK4 inhibitory activity. The inhibitory activity is further enhanced when an aryl or heteroaryl substituent is introduced at the C-6 position of the isoquinoline-1,3(2H,4H)-dione core. We present here SAR data and a CDK4 mimic model that explains the binding, potency, and selectivity of our CDK4 selective inhibitors.

Journal of Medicinal Chemistry published new progress about 55403-35-5. 55403-35-5 belongs to piperazines, auxiliary class Pyridine,Piperazine,Amine, name is 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, and the molecular formula is C12H14O2, Product Details of C10H16N4.

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

Tomishima, Masaki published the artcileNovel echinocandin antifungals. Optimization of the side chain of the natural product FR901379. Discovery of micafungin, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(9), 2886-2890, database is CAplus and MEDLINE.

Further optimization of the potent antifungal activity of side chain analogs of the natural product FR901379 led to the discovery of compound (I) with an excellent, well-balanced profile. Potent compounds with reduced hemolytic potential were designed based upon a disruption of the linearity of the terphenyl lipophilic side chain. The optimized compound I (FK463, micafungin) displayed the best balance and was selected as the clin. candidate.

Bioorganic & Medicinal Chemistry Letters published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C7H9BO3S, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

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

Byrtus, Hanna published the artcileSynthesis and anticonvulsant activity of new N-Mannich bases derived from 5-cyclopropyl-5-phenyl- and 5-cyclopropyl-5-(4-chlorophenyl)-imidazolidine-2,4-diones, Related Products of piperazines, the publication is Bioorganic & Medicinal Chemistry (2011), 19(20), 6149-6156, database is CAplus and MEDLINE.

Synthesis, physicochem. and anticonvulsant properties of new N-Mannich bases derived from 5-cyclopropyl-5-phenyl- and 5-cyclopropyl-5-(4-chlorophenyl)-imidazolidine-2,4-diones have been described. Initial anticonvulsant screening was performed using i.p. maximal electroshock (MES) and s.c. pentylenetetrazole (scPTZ) seizure tests. The neurotoxicity was determined applying the rotarod test. The in vivo results in mice showed that all compounds were effective especially in the MES screen. The quant. evaluation after oral administration in rats showed that the most active was 5-cyclopropyl-5-phenyl-imidazolidine-2,4-dione (I) with ED₅₀ values of 5.76 mg/kg (MES) and 57.31 mg/kg (scPTZ). This mol. was more potent than phenytoin and ethosuximide which were used as reference antiepileptic drugs. Addnl. compound I with ED₅₀ of 26.06 mg/kg in psychomotor seizure test (6-Hz) in mice showed comparable activity to new generation anticonvulsant – levetiracetam.

Bioorganic & Medicinal Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Related Products of piperazines.

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

Kumar, J. Ranjith published the artcileSynthesis and antimicrobial activity of new series of piperazine containing chalcone derivatives, SDS of cas: 67914-60-7, the publication is PHARMANEST (2014), 5(2), 1943-1946, database is CAplus.

Treatment of 1-acetyl-4-(4-hydroxyphenyl)piperazine with aromatic or substituted aromatic aldehydes in presence of methanol and potassium hydroxide, formed 3-substituted phenyl-1-(4-(4-hydroxylphenyl)piperzin-1-yl)-prop-2-en-1-one derivatives I (R = Ph, 4-ClC₆H₄, 4-FC₆H₄, etc.). These are assayed for their antibacterial activity against Bacillus pumilus, Bacillus subtilis, Escherichia coli, Proteus vulgaris and for antifungal activity against Aspergillus niger, Candida albicans strains. Antibacterial assay revealed that Bacillus subtilis and Proteus vulgaris were the most sensitive bacterial strains to compounds I (R = 4-ClC₆H₄, 4-FC₆H₄, 4-O₂NC₆H₄, 2,4-di-MeOC₆H₃, 2,4-Cl₂C₆H₃) and in the antifungal assay, compounds I (R = Ph, 4-FC₆H₄, 2,4-Cl₂C₆H₃) were highly effective against Aspergillus niger when compared to other other investigated strains.

PHARMANEST published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, SDS of cas: 67914-60-7.

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

Mazzei, Mauro published the artcileActivity of Mannich bases of 7-hydroxycoumarin against Flaviviridae, Quality Control of 87179-40-6, the publication is Bioorganic & Medicinal Chemistry (2008), 16(5), 2591-2605, database is CAplus and MEDLINE.

Some Mannich bases of 7-hydroxycoumarin (2) and their simple derivatives (3 and 4) were prepared and tested against viruses containing single-stranded, pos.-sense RNA genomes (ssRNA⁺). This study was directed toward Flaviviridae and, in particular, HCV surrogate viruses (BVDV, YFV). The 7-hydroxy derivatives 2 were generally devoid of activity, but when position 7 was propylated, the resulting 7-propyloxy derivatives 3 were in some cases endowed with an interesting activity against BVDV. The formation of 7-benzoyl derivatives 4 gave compounds generally lacking in activity against Flaviviridae, whereas the appearance of activity against RSV has been observed Also some unsym. methylene derivatives 5-7 (namely coumarins bridged to chromones or indoles) were found moderately active in antiviral tests. Derivatives 3 were submitted to a mol. modeling study using DNA polymerase of HCV as a target. The good correlation between calculated mol. modeling IC₅₀ and exptl. EC₅₀ indicates that DNA polymerase is potentially involved in the inhibition of surrogate HCV viruses.

Bioorganic & Medicinal Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Quality Control of 87179-40-6.

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

Salahifar, Eslam published the artcileRegioselective Green Electrochemical Approach to the Synthesis of Nitroacetaminophen Derivatives, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Organic Letters (2015), 17(19), 4666-4669, database is CAplus and MEDLINE.

A regioselective green synthesis of nitroacetaminophen derivatives e. g., I, was carried out by electrochem. oxidation of acetaminophen, N-(2-hydroxyphenyl)acetamide, and 1-(4-(4-hydroxyphenyl)piperazin-1-yl)ethanone in the presence of nitrite ion as a nucleophile. The present work has led to the development of a reagentless green and facile electrochem. method for the synthesis of some nitroacetaminophen derivatives

Organic Letters published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

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