Tag: M.W=200-250

Ryu, Jae Chun published the artcileSynthesis of ketoconazole derivatives, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Bulletin of the Korean Chemical Society (2003), 24(4), 460-466, database is CAplus.

For the drug master file (DMF) of ketoconazole, four impurities contained in ketoconazole were synthesized. During the synthesis of I, a new synthetic method of 1,4-dihydropyrazine was established. To oxidize the aminoalc. of I to the aminal I, the standard Swern oxidation condition was modified to mask the nucleophilicity of the amino group temporarily using one equivalent of acetic acid. Derivative II was synthesized via regioselective bromination at the I position of the 4-aminophenol derivative of II using Br₂ in the presence of p-TsOH. The etherification of aryl bromide with a phenol derivative compound was accomplished by a modification of the general Cu-mediated reaction condition using excess of the phenol derivative itself as a solvent at elevated temperature (190 °C).

Bulletin of the Korean Chemical Society 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

Kong, Jeong-Ok published the artcileNematicidal activity of cassia and cinnamon oil compounds and related compounds toward Bursaphelenchus xylophilus (Nematoda: Parasitaphelenchidae), Recommanded Product: (E)-1-Cinnamylpiperazine, the publication is Journal of Nematology (2007), 39(1), 31-36, database is CAplus and MEDLINE.

The nematicidal activity of two cassia, Cinnamomum cassia, oils (Especial and true), four cinnamon, Cinnamomum zeylanicum, oils (tech., #500, bark and green leaf), and their compounds (e.g., trans-cinnamaldehyde and trans-cinnamic acid) toward adult Bursaphelenchus xylophilus was examined by a direct contact bioassay. Results were compared with those of 34 related compounds As judged by 24-h LC₅₀ values, two cassia oils (0.084-0.085 mg/mL) and four cinnamon oils (0.064-0.113 mg/mL) were toxic toward adult B. xylophilus. Of 45 test compounds, trans-cinnamaldehyde (0.061 mg/mL) was the most active nematicide, followed by Et cinnamate, α-methyl-trans-cinnamaldehyde, Me cinnamate and allyl cinnamate (0.114-0.195 mg/mL). Potent nematicidal activity was also observed with 4-methoxycinnamonitrile, trans-4-methoxycinnamaldehyde, trans-2-methoxycinnamaldehyde, Et α-cyanocinnamate, cinnamonitrile and cinnamyl bromide (0.224-0.502 mg/mL). Structure-activity relationships indicate that structural characteristics, such as types of functional groups, saturation and carbon skeleton, appear to play a role in determining the toxicities to adult B. xylophilus. Cassia and cinnamon oils and test compounds described merit further study as potential nematicides or leads for the control of pine wilt disease caused by B. xylophilus.

Journal of Nematology 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, Recommanded Product: (E)-1-Cinnamylpiperazine.

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

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

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

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

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