Category: piperazines

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

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

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

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

Bachovchin, Kelly A. published the artcileImprovement of aqueous solubility of lapatinib-derived analogues: identification of a quinolinimine lead for human African trypanosomiasis drug development, Synthetic Route of 914610-39-2, the publication is Journal of Medicinal Chemistry (2019), 62(2), 665-687, database is CAplus and MEDLINE.

Lapatinib, an approved epidermal growth factor receptor inhibitor, was explored as a starting point for the synthesis of new hits against Trypanosoma brucei, the causative agent of human African trypanosomiasis (HAT). Previous work culminated in I, which was part of a series typically associated with poor aqueous solubility In this report, we present various medicinal chem. strategies that were used to increase the aqueous solubility and improve the physicochem. profile without sacrificing antitrypanosomal potency. To rank trypanocidal hits, a new assay (summarized in a cytocidal effective concentration (CEC₅₀)) was established, as part of the lead selection process. Increasing the sp³ carbon content of I resulted in II (0.19 μM EC₅₀ against T. brucei and 990 μM aqueous solubility). Further chem. exploration of II yielded III, a trypanocidal quinolinimine (EC₅₀: 0.013 μM; aqueous solubility: 880 μM; and CEC₅₀: 0.18 μM). Compound III reduced parasitemia 10⁹ fold in trypanosome-infected mice; it is an advanced lead for HAT drug development.

Journal of Medicinal Chemistry published new progress about 914610-39-2. 914610-39-2 belongs to piperazines, auxiliary class Piperazine,Boronic acid and ester,Sulfamide,Benzene,Piperazine,Boronate Esters,Boronic acid and ester,, name is 1-Methyl-4-((4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)sulfonyl)piperazine, and the molecular formula is C17H27BN2O4S, Synthetic Route of 914610-39-2.

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

Raajaraman, BR. published the artcileInvestigation on 1-Acetyl-4-(4-hydroxyphenyl) piperazine an anti-fungal drug by spectroscopic, quantum chemical computations and molecular docking studies, Application of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Journal of Molecular Structure (2018), 583-595, database is CAplus.

The title compound, 1-acetyl-4-(4-hydroxyphenyl)piperazine (1A4HP) has been examined by FT-Raman, FT-IR, ¹HNMR, ¹³CNMR and UV-Visible spectra range. By using the d. functional theory (DFT) by the method B3LYP and basis set 6-311++G(d,p) the optimized figure of 1A4HP, the vibrational modes, the IR penetration intensities and the working of Raman scattering were estimated The optimized mol. figure obtained by the DFT method and its bond length and bond angle computed values are same as the XRD exptl. values. AIM topol. anal. was done on the mol. The HOMO and LUMO energy results show that good exchange of charge happened inside the mol. NBO method was applied to study donor-acceptor interactions. ¹H and ¹³C chem. shift of NMR were estimated using the type gauge-independent AO (GIAO) and the results are related to the exptl. values. The hyperpolarizability computation shows the 1A4HP has very good NLO property. The anal. of Fukui function and Mol. electrostatic potential (MEP) studies were done. The essential thermodn. characters (entropy, enthalpy and heat capacity) of the 1A4HP estimated at various temperatures The best ligand-protein interactions are done by mol. docking with the various antifungal proteins and the ligand 1A4HP.

Journal of Molecular Structure 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, Application of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

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

Wilson, Daniel J. published the artcileA continuous fluorescence displacement assay for BioA: An enzyme involved in biotin biosynthesis, Product Details of C20H17ClN4O3, the publication is Analytical Biochemistry (2011), 416(1), 27-38, database is CAplus and MEDLINE.

Cofactor biosynthetic pathways represent a rich source of potential antibiotic targets. The second step in biotin biosynthesis is performed by BioA, a pyridoxal 5′-phosphate (PLP)-dependent enzyme. This enzyme has been confirmed as a candidate target in Mycobacterium tuberculosis; however, the current bioassay used to measure BioA activity is cumbersome and low throughput. Here we describe the design, development, and optimization of a continuous coupled fluorescence displacement assay to measure BioA activity. In this coupled assay, BioD converts the product of the BioA-catalyzed reaction into dethiobiotin, which is subsequently detected by displacement of a fluorescently labeled dethiobiotin probe from streptavidin. The assay was further adapted to a high-throughput screening format and validated against the LOPAC¹²⁸⁰ library.

Analytical Biochemistry 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 C6H8N2, Product Details of C20H17ClN4O3.

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

Itsumi, Momoe published the artcileProfile of androgen receptor activators identified using high-throughput screen, Recommanded Product: 2-((4-(4-Chlorophenyl)piperazin-1-yl)methyl)pyrazolo[1,5-a]pyridine, the publication is Andrologia (2021), 53(1), e13856, database is CAplus and MEDLINE.

In this study using distinct system, effectors on dopamine signalling were identified as candidates that prominently increase AR activity. Then, this study suggested novel function on AR signalling in several compounds, which may be useful or harmful in organs where AR signalling play a role. In conclusion, various candidates for AR activation were identified using high-throughput screening.

Andrologia published new progress about 337972-47-1. 337972-47-1 belongs to piperazines, auxiliary class Inhibitor, name is 2-((4-(4-Chlorophenyl)piperazin-1-yl)methyl)pyrazolo[1,5-a]pyridine, and the molecular formula is C18H19ClN4, Recommanded Product: 2-((4-(4-Chlorophenyl)piperazin-1-yl)methyl)pyrazolo[1,5-a]pyridine.

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

Deng, Yongqi published the artcileDiscovery of Novel, Dual Mechanism ERK Inhibitors by Affinity Selection Screening of an Inactive Kinase, COA of Formula: C16H18N2, the publication is Journal of Medicinal Chemistry (2014), 57(21), 8817-8826, database is CAplus and MEDLINE.

An affinity-based mass spectrometry screening technol. was used to identify novel binders to both nonphosphorylated and phosphorylated ERK2. Screening of inactive ERK2 identified a pyrrolidine analog 1 that bound to both nonphosphorylated and phosphorylated ERK2 and inhibited ERK2 kinase activity. Chem. optimization identified compound 4 as a novel, potent, and highly selective ERK1,2 inhibitor which not only demonstrated inhibition of phosphorylation of ERK substrate p90RSK but also demonstrated inhibition of ERK1,2 phosphorylation on the activation loop. X-ray cocrystallog. revealed that upon binding of compound 4 to ERK2, Tyr34 undergoes a rotation (flip) along with a shift in the poly-Gly rich loop to create a new binding pocket into which 4 can bind. This new binding mode represents a novel mechanism by which high affinity ATP-competitive compounds may achieve excellent kinase selectivity.

Journal of Medicinal Chemistry published new progress about 180698-19-5. 180698-19-5 belongs to piperazines, auxiliary class Piperazine,Benzene, name is 1-Biphenyl-4-yl-piperazine, and the molecular formula is C16H18N2, COA of Formula: C16H18N2.

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

Malinka, W. published the artcileSynthesis and preliminary screening of derivatives of 2-(4-arylpiperazin- 1-ylalkyl)-3-oxoisothiazolo[5,4-b]pyridines as CNS and antimycobacterial agents, Application In Synthesis of 87179-40-6, the publication is Pharmazie (2000), 55(6), 416-425, database is CAplus and MEDLINE.

Isothiazolopyridines, e.g. I (X = S, SO₂; X¹ = CO, CH₂CH₂, CH₂CH₂CH₂; R = H, 3-Cl, 3-CF₃, 2-MeO), were prepared that possess a side chain at the isothiazole ring typical, among others, for trazodone or NAN-195. Representatives of these novel isothiazolopyridines were examined for acute toxicity and in several commonly used CNS tests in mice and for arterial blood pressure in rats. Three of the five compounds tested showed significant analgesic activity. The most active compound, I (X = S; X¹ = CH₂CH₂; R = 3-Cl) exhibited analgesic action in the writhing test in a dose 1/1280 of LD₅₀ (LD₅₀ = 1135.5 mg/kg) after administration i.p. to mice. Addnl., the compounds described here and related isothiazolopyridines obtained previously were evaluated against Mycobacterium tuberculosis H₃₇Rv at 12.5 μg/mL in in vitro assays. Seven of the nineteen compounds tested showed 100% inhibition of that mycobacterium.

Pharmazie 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, Application In Synthesis of 87179-40-6.

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