Month: November 2022

Kavitha, Channappa N. published the artcile1-[4-(4-Hydroxyphenyl)piperazin-1-yl]ethanone, Quality Control of 67914-60-7, the publication is Acta Crystallographica, Section E: Structure Reports Online (2013), 69(11), o1671, database is CAplus and MEDLINE.

In the title compound, C₁₂H₁₆N₂O₂, the piperazine ring has a chair conformation. The dihedral angle between the mean planes of the benzene ring and the acetyl group is 48.7 (1)°. In the crystal, mols. are linked via O-H···O hydrogen bonds, forming chains propagating along [010].

Acta Crystallographica, Section E: Structure Reports Online 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, Quality Control of 67914-60-7.

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

Nguyen, William published the artcileOptimization of 5-substituted thiazolyl ureas and 6-substituted imidazopyridines as potential HIV-1 latency reversing agents, Computed Properties of 178928-58-0, the publication is European Journal of Medicinal Chemistry (2020), 112254, database is CAplus and MEDLINE.

Here, two strategies to further improve the activation of viral gene expression and physicochem. properties of this class was implemented. Firstly, rigidification of the central oxy-carbon linker with a variety of saturated heterocycles and secondly, investigated bioisosteric replacement of the 2-acylaminothiazole moiety was explored. The optimization process afforded lead compounds, imidazopyridine derivatives such as I from the 2-piperazinyl thiazolyl urea and the imidazopyridine class. The imidazopyridine derivatives from each class demonstrated potent activation of HIV gene expression in the FlpIn. FM HEK293 cellular assay (both with LTR EC₅₀s of 80 nM) and in the Jurkat Latency 10.6 cell model (LTR EC₅₀ 220 and 320 nM resp.), but consequently activated gene expression non-specifically in the FlpIn. FM HEK293 cellular assay (CMV EC₅₀ 70 and 270 nM resp.) manifesting in cellular cytotoxicity. The lead compounds had potential for further development as novel latency reversing agents.

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, Computed Properties of 178928-58-0.

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

Sanjeevarayappa, C. published the artcileDesign, synthesis, characterization and biological evaluation of novel amides containing 1,2,4-oxadiazole derivatives, Product Details of C10H17N3O2, the publication is Journal of Applicable Chemistry (Lumami, India) (2014), 3(1), 38-46, 9 pp., database is CAplus.

Some new amides containing oxadiazole derivatives, I (R = 2,3-F₂C₆H₃, 2,4-Cl₂C₆H₃, c-C₆H₁₁, 1-methyl-2-indolyl, etc.), have been synthesized using N-Boc piperazine as starting material. The latter was converted to N-cyano-4-Boc piperazine by nucleophilic substitution reaction. The substituted product was treated with hydroxylamine hydrochloride under basic conditions to give the hydroxycarbamimide and was cyclized with 3-fluorobenzoic acid to yield N-protected piperazinyl-1,2,4-oxadiazole. Deprotection of the secondary amine was done using trifluoroacetic acid; the free amine was then condensed with different substituted acids, RCO₂H, in the presence of triethylamine to yield the title compounds All the synthesized compounds were screened for their in vitro antibacterial activity and anthelmintic activity. Some of the compounds showed good biol. activity.

Journal of Applicable Chemistry (Lumami, India) published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, Product Details of C10H17N3O2.

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

Waltemate, Jana published the artcile10-(4-Phenylpiperazine-1-carbonyl)acridin-9(10H)-ones and related compounds: Synthesis, antiproliferative activity and inhibition of tubulin polymerization, Related Products of piperazines, the publication is Bioorganic & Medicinal Chemistry Letters (2021), 127687, database is CAplus and MEDLINE.

As part of our continuing search for potent inhibitors of tubulin polymerization, two novel series of 42 10-(4-phenylpiperazine-1-carbonyl)acridin-9(10H)-ones and N-benzoylated acridones were synthesized on the basis of a retrosynthetic approach. All newly synthesized compounds were tested for antiproliferative activity and interaction with tubulin. Several analogs potently inhibited tumor cell growth. Among the compounds tested, 10-(4-(3-methoxyphenyl)piperazine-1-carbonyl)acridin-9(10H)-one (17c, I) exhibited excellent growth inhibitory effects on 93 tumor cell lines, with an average GI₅₀ value of 5.4 nM. We were able to show that the strong cytotoxic effects are caused by disruption of tubulin polymerization, as supported by the EBI (N,N’-Ethylenebis(iodoacetamide)) assay and the fact that the most potent inhibitors of cancer cell growth turned out to be the most efficacious tubulin polymerization inhibitors. Potencies were nearly comparable or superior to those of the antimitotic reference compounds Closely related to this, the most active analogs inhibited cell cycling at the G2/M phase at concentrations down to 30 nM and induced apoptosis in K562 leukemia cells. We believe that our work not only proves the excellent suitability of the acridone scaffold for the design of potent tubulin polymerization inhibitors but also enables synthetic access to further potentially interesting N-acylated acridones.

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 C8H8O3, Related Products of piperazines.

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

Degirmencioglu, Ismail published the artcileSynthesis of axially disubstituted silicon(IV) phthalocyanines and investigation of their photophysical and photochemical properties, HPLC of Formula: 67914-60-7, the publication is Journal of Molecular Structure (2022), 131599, database is CAplus.

In this study, the axially 1-(4-(3-(6-hydroxyhexyl)-3,4-dihydro-2H-benzo[e][1,3]oxazin-6-yl)piperazin-1-yl)ethanone and 1-(4-(3-(2-(2-hydroxyethoxy)ethyl)-3,4-dihydro-2H-benzo[e][1,3]oxazin-6-yl)piperazin-1-yl)ethanone disubstituted silicon(IV) phthalocyanines and their corresponding quaternized derivatives were synthesized for the first time as candidate photosensitizers for photodynamic therapy (PDT) in cancer treatment. The structures of these novel compounds were confirmed by some spectroscopic techniques such as FT-IR, ¹H NMR, ¹³C NMR, UV-Vis, and mass. The axially substitution increased the solubility of the silicon(IV) phthalocyanines. The prepared silicon(IV) phthalocyanines showed great results achieved from photochem. and photophys. investigations in DMSO solution Especially, high singlet oxygen and the fluorescence quantum yield values of the quaternized silicon (IV) phthalocyanines indicates that these compounds have major potential as photosensitizers in PDT. Furthermore, studied silicon(IV) phthalocyanine complexes could be classified as the stable photosensitizer in accordance with photodegradation study results. The fluorescence quenching behavior of these phthalocyanine complexes was also examined using fluorescence quenching method by 1,4-benzoquinone (BQ).

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, HPLC of Formula: 67914-60-7.

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

Abbasi, Muhammad Athar published the artcileSynthesis of some N-sulfonated derivatives of 1-[(E)-3-phenyl-2-propenyl]piperazine as suitable antibacterial agents, HPLC of Formula: 87179-40-6, the publication is Pakistan Journal of Pharmaceutical Sciences (2020), 33(4), 1609-1616, database is CAplus.

In the planned research work, the nucleophilic substitution reaction of 1-[(E)-3-phenyl-2-propenyl]piperazine was carried out with different sulfonyl chlorides at pH 9-10 to synthesize its different N-sulfonated derivatives The inhibition potential of the synthesized mols. was ascertained against two bacterial pathogenic strains i.e., Bacillus subtilis and Escherichia coli. It was inferred from the results that some of the compounds were very suitable inhibitors of these bacterial strains. Their cytotoxicity profile was also studied through hemolytic study.

Pakistan Journal of Pharmaceutical Sciences 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, HPLC of Formula: 87179-40-6.

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

Loeber, Stefan published the artcileRationally Based Efficacy Tuning of Selective Dopamine D4 Receptor Ligands Leading to the Complete Antagonist 2-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213), Related Products of piperazines, the publication is Journal of Medicinal Chemistry (2001), 44(17), 2691-2694, database is CAplus and MEDLINE.

Structure dependent efficacy studies in the field of selective D4 ligands led to the 2-aminomethyl substituted azaindole 2 (FAUC 213) that displayed strong D4 binding, high subtype selectivity, and complete antagonist properties in ligand-induced mitogenesis experiments According to our schematic mol. model, the intrinsic activity of the regioisomers investigated is controlled by the ability of the heterocyclic unit to interact with both elements of the D4 binding-site crevice, the aromatic microdomain in TM6, and a serine residue in TM5.

Journal of Medicinal Chemistry 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, Related Products of piperazines.

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

Yu, Lei published the artcileA structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFR^L858R/T790M mutant with improved pharmacokinetic properties, Recommanded Product: 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, the publication is European Journal of Medicinal Chemistry (2017), 1107-1117, database is CAplus and MEDLINE.

Structural optimization of pyrido[2,3-d]pyrimidin-7-ones was conducted to yield a series of new selective EGFR^T790M inhibitors with improved pharmacokinetic properties. One of the most promising compound 9s (N-(3-(2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl)-5-(trifluoromethyl)phenyl)acrylamide) potently suppressed EGFR^L858R/T790M kinase and inhibited the proliferation of H1975 cells with IC₅₀ values of 2.0 nM and 40 nM, resp. The compound dose-dependently induced reduction of the phosphorylation of EGFR and downstream activation of ERK in NCI-H1975 cells. It also exhibited moderate plasma exposure after oral administration and an oral bioavailability value of 16%. Compound 9s may serve as a promising lead compound for further drug discovery overcoming the acquired resistance of non-small cell lung cancer (NSCLC) patients.

European 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 C15H14O, Recommanded Product: 6-(4-Methylpiperazin-1-yl)pyridin-3-amine.

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

Jiang, Xiong-Jie published the artcilePreparation and in vitro photodynamic activities of novel axially substituted silicon (IV) phthalocyanines and their bovine serum albumin conjugates, Formula: C12H16N2O2, the publication is Bioorganic & Medicinal Chemistry Letters (2006), 16(9), 2450-2453, database is CAplus and MEDLINE.

Two novel axially substituted phthalocyanines, namely bis(4-(4-acetylpiperazine)phenoxy)phthalocyaninatosilicon (IV) (1) and its N-methylated derivative 2, have been synthesized. The dicationic phthalocyanine 2 is non-aggregated in water and exhibits good photophys. properties. The non-covalent BSA conjugates of these compounds have also been prepared Compound 2 and the conjugate 2-BSA show extremely high photodynamic activities toward B16 melanoma cancer cell lines. The corresponding 50% growth-inhibitory (IC₅₀) ratios are 33 and 38 nM, resp.

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 C12H16N2O2, Formula: C12H16N2O2.

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

Yu, Le-Mao published the artcileSynthesis and structure-activity relationship of furoquinolinediones as inhibitors of Tyrosyl-DNA phosphodiesterase 2 (TDP2), Related Products of piperazines, the publication is European Journal of Medicinal Chemistry (2018), 777-796, database is CAplus and MEDLINE.

Tyrosyl-DNA phosphodiesterase 2 (TDP2) is a recently discovered enzyme specifically repairing topoisomerase II (TOP2)-mediated DNA damage. It has been shown that inhibition of TDP2 synergize with TOP2 inhibitors. Herein, we report the discovery of the furoquinolinedione chemotype as a suitable skeleton for the development of selective TDP2 inhibitors. Compound 1 was identified as a TDP2 inhibitor as a result of screening our inhouse compound library for compounds selective for TDP2 vs. TDP1. Further SAR studies provide several selective TDP2 inhibitors at low-micromolar range. The most potent compound 74 shows inhibitory activity with IC₅₀ of 1.9 and 2.1 μM against recombinant TDP2 and TDP2 in whole cell extracts (WCE), resp.

European Journal of Medicinal Chemistry 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 C11H9NO3, Related Products of piperazines.

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