Month: November 2022

Irie, Osamu published the artcileDiscovery of Orally Bioavailable Cathepsin S Inhibitors for the Reversal of Neuropathic Pain, Synthetic Route of 67914-60-7, the publication is Journal of Medicinal Chemistry (2008), 51(18), 5502-5505, database is CAplus and MEDLINE.

Cathepsin S inhibitors are well-known to be an attractive target as immunol. therapeutic agents. Recently, our gene expression anal. identified that cathepsin S inhibitors could also be effective for neuropathic pain. Herein, we describe the efficacy of selective cathepsin S inhibitors as antihyperalgesics in a model of neuropathic pain in rats after oral administration.

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, Synthetic Route of 67914-60-7.

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

Yoneyama, Hiroshi published the artcileStudies on antimicrobial activity of ketoconazole (KW-1414). VI. In vitro antifungal and antibacterial activity of ketoconazole (KW-1414) and its analogs, Synthetic Route of 67914-60-7, the publication is Shinkin to Shinkinsho (1984), 25(4), 372-8, database is CAplus.

Antifungal activities of structural analogs and metabolites of the synthetic antifungal agent ketoconazole (KCZ; KW-1414) (I) were investigated. R-39519 (desacetyl derivative) and R-44319 (trans isomer) had less antifungal activity against Candida species and dermatophytes than did I. HLI-151 (oxidized derivative) had no antifungal activity against any of the yeasts or fungi. Two known physiol. metabolites of I, R-43568 and T-1141, also showed no antifungal activity. I, R-39519, R-43568, and T-1141 showed no antibacterial activity against 12 strains of Lactobacillus species which are normal flora of the vagina. In blood of human volunteers administered orally 200 mg of I, no antifungal activity was detected except for I by bioautog. seeded with Kluyveromyces fragilis. In human urine of the same volunteers, no antifungal activity was detected by the bioautog.

Shinkin to Shinkinsho 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 C14H10O4S2, Synthetic Route of 67914-60-7.

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

Kumar, Nilesh published the artcileSmall-Molecule Diversity Using a Skeletal Transformation Strategy, HPLC of Formula: 87179-40-6, the publication is Organic Letters (2005), 7(13), 2535-2538, database is CAplus and MEDLINE.

A short synthetic sequence resulting in >4000 skeletally diverse small mols. that have three distinct skeletal frameworks among other unique structural features is described. The sequence entails skeletal transformations pioneered by Winterfeldt and co-workers. The following reaction sequence is used: epoxide ring opening and subsequent functionalization that provide, e.g., spirocyclic oxazolidines, Lewis acid catalyzed Diels-Alder cycloaddition of steroid-derived dienes with ynones, and subsequent retro-Diels-Alder fragmentation that yields 14-membered paracyclophanes.

Organic 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, HPLC of Formula: 87179-40-6.

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

Na, Young Eun published the artcileFumigant toxicity of cassia and cinnamon oils and cinnamaldehyde and structurally related compounds to Dermanyssus gallinae (Acari: Dermanyssidae), Quality Control of 87179-40-6, the publication is Veterinary Parasitology (2011), 178(3-4), 324-329, database is CAplus and MEDLINE.

The toxicity of two cassia oils, four cinnamon oils and (E)-cinnamaldehyde and (E)-cinnamic acid and 34 structurally related compounds to adult Dermanyssus gallinae (De Geer) collected from a poultry house was examined using a vapor-phase mortality bioassay. Results were compared with those of dichlorvos, a conventional acaricide. The cassia and cinnamon oils (cinnamon tech., cinnamon #500, cassia especial, cassia true, cinnamon bark and cinnamon green leaf) exhibited good fumigant toxicity (LD₅₀, 11.79-26.40 μg cm^-3). α-Methyl-(E)-cinnamaldehyde (LD₅₀, 0.45 μg cm^-3) and (E)-cinnamaldehyde (0.54 μg cm^-3) were the most toxic compounds and the toxicity of these compounds was comparable to that of dichlorvos (0.30 μg cm^-3). Potent fumigant toxicity was also observed in allyl cinnamate, ethyl-α-cyanocinnamate, (E)-2-methoxylcinnamic acid and (Z)-2-methoxylcinnamic acid (LD₅₀, 0.81-0.92 μg cm^-3). Structure-activity relationships indicate that structural characteristics, such as types of functional groups and carbon skeleton rather than vapor pressure parameter, appear to play a role in determining toxicity. The essential oils and compounds described merit further study as potential acaricides for the control of D. gallinae populations as fumigants with contact action due to global efforts to reduce the level of highly toxic synthetic acaricides in the agricultural environment.

Veterinary Parasitology 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

Lee, Eun-Jeong published the artcileToxicity of cassia and cinnamon oil compounds and cinnamaldehyde-related compounds to Sitophilus oryzae (Coleoptera: Curculionidae), Recommanded Product: (E)-1-Cinnamylpiperazine, the publication is Journal of Economic Entomology (2008), 101(6), 1960-1966, database is CAplus and MEDLINE.

The toxicity to adult Sitophilus oryzae (L.) (Coleoptera: Curculionidae) of two cassia oils (Especial and true), four cinnamon oils (tech., #500, bark, and green leaf), and (E)-cinnamaldehyde and its 41 structurally related compounds was examined by residual and vapor-phase toxicity bioassays. Results were compared with those of dichlorvos. In residual bioassays, cassia and cinnamon oils exhibited good insecticidal activity. Based on 48-h LD₅₀ values, the toxicity of allyl cinnamate (0.0003 mg/cm²) was comparable with that of dichlorvos (0.00025 mg/cm²). Potent insecticidal activity also was observed with benzaldehyde, β-caryophyllene, cinnamonitrile, hydrocinnamyl acetate, (E)-4-hydroxycinnamic acid, and α-terpineol (LD₅₀ = 0.003-0.009 mg/cm²). Structure-activity relationships indicate that types of functional groups rather than hydrophobicity or vapor pressure parameters seem to play a role in determining the toxicities to adult S. oryzae. In vapor-phase toxicity tests with weevils, these compounds were more effective in closed containers than in open ones. These results indicate that the effect of the compounds was largely a result of action in the vapor phase. Cassia and cinnamon oils and test compounds described merit further study as potential fumigants for the control of S. oryzae because of their greater activity as a fumigant.

Journal of Economic Entomology 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

Huang, Liang-Fu published the artcileSynthesis of 1,2,4-triazole and thiazole analogs of ketoconazole, Product Details of C12H16N2O2, the publication is Journal of Heterocyclic Chemistry (1997), 34(2), 469-476, database is CAplus.

The synthesis of 1,2,4-triazole and thiazole analogs of ketoconazole is described in which one of the α azole ring carbons is linked to C-2 of the ketal by means of a three methylene tether. Lithiation of 1-methyl-1,2,4-triazole and thiazole and subsequent alkylation with 2-(2,4-dichlorophenyl)-2-(3-iodopropyl)-1,3-dioxolane produced, after an aqueous acidic workup, 2,4-dichlorophenyl 3-[5-(1-methyl-1,2,4-triazolyl) and 2-thiazolyl]propyl ketones, resp. Ketalization with glycerol furnished the corresponding diastereomeric pairs of cis- and trans-1,3-dioxolanes. The reaction of 2,4-dichlorophenyl 3-[5-(1-methyl-1,2,4-triazolyl)]propyl ketone with 3-mercapto-1,2-propanediol produced the corresponding diastereomeric cis- and trans-hydroxymethyl-1,3-oxathiolanes. The diastereomeric racemates were separated by column chromatog. and their stereochem. established by NOE NMR experiments Some of these racmic cis ketal alcs. were converted by benzyl bromide to the corresponding benzyl ethers. Several of these racemic cis-ketals were reacted, first with methanesulfonyl chloride, then with 1-acetyl-4-(4-hydroxyphenyl)piperazine, to furnish the title compounds

Journal of Heterocyclic 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, Product Details of C12H16N2O2.

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

Wang, Zhangqian published the artcileContact and fumigant toxicity of cinnamaldehyde and cinnamic acid and related compounds to Dermatophagoides farinae and Dermatophagoides pteronyssinus (Acari: Pyroglyphidae), Synthetic Route of 87179-40-6, the publication is Journal of Medical Entomology (2011), 48(2), 366-371, database is CAplus and MEDLINE.

Toxicities of (E)-cinnamaldehyde and (E)-cinnamic acid and their 41 structurally related compounds to adult Dermatophagoides farinae Hughes and Dermatophagoides pteronyssinus Trouessart (Acari: Pyroglyphidae) were examined using fabric-circle contact plus fumigant and vapor-phase mortality bioassays. Results were compared with those of two acaricides, benzyl benzoate and di-Bu phthalate. In contact plus fumigant mortality bioassays, the most toxic compounds were (E)-cinnamaldehyde, Me (E)-cinnamate, cinnamyl acetate, and hydrocinnamaldehyde against adult D. farinae (17.5-23.3 mg/m²) and D. pteronyssinus (19.0-24.0 mg/m²), based on 24-h 50% lethal concentration (LC₅₀) values. These compounds were significantly more toxic than either benzyl benzoate (LC₅₀, 64.9 and 60.5 mg/m²) or di-Bu phthalate (218.9 and 232.3 mg/m²). The toxicity of allyl cinnamate vs. benzyl benzoate was not significantly different. Structure-activity relationship indicates that structural characteristics, such as types of functional groups, carbon skeleton, and saturation, appear to play a role in determining the compound toxicities. In vapor-phase mortality bioassays, these compounds were effective against adult D. farinae in closed, but not in open containers, indicating that their mode of delivery was largely a result of vapor action. The active compounds described merit further study as potential house dust mite control fumigants with contact action in light of global efforts to reduce the level of highly toxic synthetic acaricides in indoor environments.

Journal of Medical Entomology 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 C14H20BClO2, Synthetic Route of 87179-40-6.

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

Lee, Chi-Hoon published the artcileAcaricidal properties of piperazine and its derivatives against house-dust and stored-food mites, Synthetic Route of 87179-40-6, the publication is Pest Management Science (2009), 65(6), 704-710, database is CAplus and MEDLINE.

Piperazine derivatives possess pharmacol. properties, yet the acaricidal activity of these compounds has not been investigated. This study was conducted to evaluate the color alteration and acaricidal activity of piperazine derivatives against Dermatophagoides spp. and Tyrophagus putrescentiae using filter paper and fumigant methods. In a fumigant bioassay, 1-phenylpiperazine (7.83 μg/cm²) against D. farinae was found to be 4.7-fold more toxic than DEET (36.84 μg/cm²), followed by benzyl benzoate (9.72 μg/cm²), piperazine (11.41 μg/cm²), 1-ethoxycarbonylpiperazine (20.14 μg/cm²), and 1-(2-methoxyphenyl)piperazine (22.14 μg/cm²). In a filter paper bioassay, 1-(2-methoxyphenyl)piperazine (3.65 μg/cm²) was 5.7-fold more toxic than DEET (20.64 μg/cm²), followed by 1-ethoxycarbonylpiperazine (4.02 μg/cm²), 1-phenylpiperazine (4.75 μg/cm²), benzyl benzoate (7.83 μg/cm²), and piperazine (10.59 μg/cm²). Similar results have been exhibited with piperazine derivatives against D. pteronyssinus. However, no activity against T. putrescentiae was observed for piperazine derivatives, except for piperazine. These results indicate that piperazine derivatives may be suitable as vapor-phase acaricide fumigants owing to their high volatility, acaricidal activity and safety. 1-Phenylpiperazine was found to be an excellent mite indicator based on the color change it induced. Taken together, these findings indicate that piperazine derivatives may be used to replace existing problematical acaricides owing to their activity and ability to act as a mite indicator.

Pest Management Science 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, Synthetic Route of 87179-40-6.

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

Amani, Amene published the artcileElectrochemical oxidation of 4-(piperazin-1-yl)phenols in the presence of indole derivatives: The unique regioselectivity in the synthesis of highly conjugated bisindolyl-p-quinone derivatives, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Journal of Electroanalytical Chemistry (2012), 36-41, database is CAplus.

The electrochem. oxidation of 4-(piperazin-1-yl)phenols were studied in the presence of indole derivatives as nucleophiles in H₂O/MeCN mixture by cyclic voltammetry and controlled-potential coulometry. The reaction mechanism is believed to be oxidation of 4-(piperazin-1-yl)phenols, Michael addition reaction, oxidation of the formed adduct, another Michael addition reaction, oxidation of new adduct and hydrolysis (ECECEC). Bisindolyl-p-quinones were synthesized through the regioselective addition of indoles to electrochem. generated quinone imines in good yields at C electrode in a divided cell.

Journal of Electroanalytical 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, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

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

Amani, Amene published the artcileElectrochemical oxidation of acetaminophen and 4-(piperazin-1-yl)phenols in the presence of 4-hydroxy-1-methyl-2(1H)-quinolone, Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Journal of the Electrochemical Society (2013), 160(1), H33-H40, database is CAplus.

A facile and 1-pot electrochem. method for the synthesis of mono and disubstituted 1,4-benzoquinones generated from the electrochem. oxidation of 1-(4-(4-hydroxyphenyl)piperazin-1-yl)ethanone (1a), 4-(piperazin-1-yl)phenol (1b) and acetaminophen (8) in the presence of 4-hydroxy-1-methyl-2(1H)-quinolone (3) as nucleophile is reported. The electrochem. generated electrophiles derived from the oxidation of 1a, 1b and 8 participate in Michael-addition reactions with 3. The authors report the synthesis of mono and diquinolone substituted of 1,4-benzoquinone in good yields based on controlled potential condition at C electrode in a divided cell.

Journal of the Electrochemical 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, Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

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