Category: piperazines

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

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

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

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

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

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

Bachovchin, Daniel A. published the artcileSuperfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening, Category: piperazines, the publication is Proceedings of the National Academy of Sciences of the United States of America (2010), 107(49), 20941-20946, S20941/1-S20941/172, database is CAplus and MEDLINE.

Serine hydrolases (SHs) are-one of the largest and most diverse enzyme classes in mammals. They play fundamental roles in virtually all physiol. processes and are targeted by drugs to treat diseases such as diabetes, obesity, and neurodegenerative disorders. Despite this, we lack biol. understanding for most of the 110+ predicted mammalian metabolic SHs, in large part because of a dearth of assays to assess their biochem. activities and a lack of selective inhibitors to probe their function in living systems. We show here that the vast majority (>80%) of mammalian metabolic SHs can be labeled in proteomes by a single, active site-directed fluorophosphonate probe. We exploit this universal activity-based assay in a library-vs.-library format to screen 70+ SHs against 140+ structurally diverse carbamates. Lead inhibitors were discovered for ∼40% of the screened enzymes, including many poorly characterized SHs: Global profiles identified carbamate inhibitors that discriminate among highly sequence-related SHs and, conversely, enzymes that share inhibitor sensitivity profiles despite lacking sequence homol. These findings indicate that sequence relatedness is not a strong predictor of shared pharmaol. within the SH superfamily. Finally, we show that lead carbamate inhibitors can be optimized into pharmacol. probes that inactivate individual SHs with high specificity in vivo.

Proceedings of the National Academy of Sciences of the United States of America 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, Category: piperazines.

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

Cramer, Richard D. published the artcile“Lead Hopping”. Validation of Topomer Similarity as a Superior Predictor of Similar Biological Activities, Safety of 2-((4-(4-Chlorophenyl)piperazin-1-yl)methyl)pyrazolo[1,5-a]pyridine, the publication is Journal of Medicinal Chemistry (2004), 47(27), 6777-6791, database is CAplus and MEDLINE.

Two extensive studies quantifying the ability of topomer shape similarity to forecast a variety of biol. similarities are described. In a prospective trial of “lead hopping”, using topomer similarity for virtual screening and queries from the patent literature, biol. assays of 308 selected compounds (representing 0.03% of those available, per assay type) yielded 11 successful “lead hops” in the 13 assays attempted. The hit rate averaged over all assays was 39% (“activity” defined as inhibition ≥20% at 10 μM), significantly greater than an unexpectedly high neg. control hit rate of 15%. The average “Tanimoto 2D fingerprint similarity” between query and “lead hop” structures (0.36) was little more than the Tanimoto similarity between random drug-like structures. Topomer shape and Tanimoto 2D fingerprint similarities were also compared retrospectively, in their tendencies to concentrate together potential and actual drugs reported to belong to the same “activity class”, for twenty classes. Among the most similar 3% of structures (corresponding to “≥0.85 Tanimoto” for these structures), an average of 62% of the topomer similar selection possessed a near neighbor belonging to the same activity class, roughly a one-third superiority over the “Tanimoto ≥ 0.85” selection containing 48% actives in avoiding false positives. Conversely, the least similar 75% of structures contained 0.3% actives for topomer similarity vs. 1.0% actives for Tanimoto 2D fingerprint similarity, a 3-fold superiority for topomers in avoiding false negatives.

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, Safety of 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

Ramesh, Deepthi published the artcileIndole chalcones: Design, synthesis, in vitro and in silico evaluation against Mycobacterium tuberculosis, Application of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is European Journal of Medicinal Chemistry (2020), 112358, database is CAplus and MEDLINE.

Indole chalcones were designed and synthesized as a promising set of compounds against H₃₇Rv strain of Mycobacterium tuberculosis. Within this library of compounds, (E)-1-(furan-3-yl)-3-(1H-indol-3-yl)prop-2-en-1-one (18), (E)-3-(1H-indol-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one (20) and (E)-2-((1H-indol-2-yl)methylene)cyclopentan-1-one (24) displayed high anti-tubercular activity at 50 μg/mL with MIC values of 210, 197 and 236 μM resp. The in-silico studies revealed that compound 18 exhibit binding modes similar to FAS-II inhibitors like INH or Thiolactomycin against KasA protein. Cytotoxicity assay results suggest that the compounds 18, 20 and 24 are non-cytotoxic to human megakaryocytes and murine B cells.

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 C12H16N2O2, Application of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

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

Harding, John R. published the artcileDevelopment of a microwave-enhanced isotopic labeling procedure based on the Eschweiler-Clarke methylation reaction, Application of (E)-1-Cinnamylpiperazine, the publication is Tetrahedron Letters (2002), 43(52), 9487-9488, database is CAplus.

A number of primary and secondary amines have been rapidly methylated under microwave-enhanced conditions using formic acid-formaldehyde mixtures, providing a route to ²H(D)-containing compounds and the potential for ³H(T), ¹¹C, ¹³C, and ¹⁴C labeling.

Tetrahedron Letters 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 of (E)-1-Cinnamylpiperazine.

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