Month: November 2022

Guo, Jia-Lin published the artcileSynthesis and biological evaluation of 3-(piperidin-4-yl)isoxazolo[4,5-d]pyrimidine derivatives as novel PI3K¦Ä inhibitors, Recommanded Product: 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, the publication is Chinese Chemical Letters (2015), 26(10), 1283-1288, database is CAplus.

An efficient synthesis of novel 3-(piperidin-4-yl)isoxazolo[4,5-d]pyrimidine scaffold has been designed and developed. A series of 5-phenylurea derivatives I [R¹ = H, CH₂CH₂NMe₂, iso-Pr, etc.; R² = Bn, H, or Et] were synthesized using this method. Their cytotoxic activities against breast cancer cell line BT-474 were evaluated by CCK-8 assay. Most of them showed potent anti-proliferative activities, of which compound 20 (I, R¹ = CH₂CH₂F and R² = Bn) and 21 (I, R¹ = Me and R² = Bn) exhibited IC₅₀s of 1.565 and 1.311 ¦ÌM, resp. Furthermore, compound 20 and 21 also showed potent inhibitory activities against PI3K¦Ä with IC₅₀s of 0.286 and 0.452 ¦ÌM, resp. These results indicate that these 3-(piperidin-4-yl)isoxazolo[4,5-d]pyrimidine derivatives are novel antitumor agents through the inhibition of PI3K¦Ä.

Chinese Chemical Letters 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 C10H16N4, Recommanded Product: 6-(4-Methylpiperazin-1-yl)pyridin-3-amine.

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

Cheng, Xian-Chao published the artcileDesign, synthesis, and biological activities of novel Ligustrazine derivatives, Related Products of piperazines, the publication is Bioorganic & Medicinal Chemistry (2007), 15(10), 3315-3320, database is CAplus and MEDLINE.

A series of novel Ligustrazine derivatives was designed, synthesized, and assayed for their protective effects on damaged ECV-304 cells and antiplatelet aggregation activities. The results showed that most Ligustrazine derivatives exhibited lower EC₅₀ values for protective effects on the ECV-304 cells damaged by hydrogen peroxide in comparison with Ligustrazine. And some Ligustrazine derivatives presented better antiplatelet aggregation activities than Ligustrazine. The derivatives containing the bisphenylmethyl pharmacophore (7a-c) exhibited highest potency. Compound 7a displayed most potential protective effects on the ECV-304 cells damaged by hydrogen peroxide, and compound 7c was found to be the most active antiplatelet aggregation agent. Structure-activity relationships were briefly discussed.

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, Related Products of piperazines.

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

Yang, Jiqiu published the artcileSynthesis of an antifungal drug ketoconazole, Application In Synthesis of 67914-60-7, the publication is Yiyao Gongye (1984), 1-4, database is CAplus.

The title compound [I, R = p-(4-acetylpiperazin-1-yl)phenyl] was prepared by condensation of I (R = MeSO₂) with piperazine II which was prepared starting from piperazine.

Yiyao Gongye 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 C24H12, Application In Synthesis of 67914-60-7.

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

Huang, Jian-Dong published the artcileTetra-(acetyl piperazine phenoxy) phthalocyaninato zinc complexes and their proteins conjugates: synthesis, characterisation and photodynamic activities, Computed Properties of 67914-60-7, the publication is Wuji Huaxue Xuebao (2006), 22(3), 435-442, database is CAplus.

Two zinc phthalocyanines, tetra-¦Á-[4-(4-acetyl piperazine) phenoxy] phthalocyaninato zinc (C₈₀H₇₂N₁₆O₈Zn) and tetra-¦Â-[4-(4-acetyl piperazine) phenoxy] phthalocyaninato zinc (C₈₀H₇₂N₁₆O₈Zn), have been synthesized and characterized with ¹H NMR, MS, IR and elemental anal. The electronic absorption spectra of two complexes in common organic solvents (N,N-DMF, THF, n-octanol) were typical for nonaggregated phthalocyanines, showing a Q band at 693?698 nm for 1 and 681 ? 682 nm for 2. This indicates that the Q band of zinc phthalocyanine with the substituted groups located in the ¦Á position is largely red shifted than that in the ¦Â position. The spectral features of complexes 1 and 2 in aqueous media suggest the ¦Á-substituted groups are more effective than ¦Â-substituted groups to hinder the aggregation of phthalocyanine mol. The interactions between two complexes with serum albumin and transferrin (BSA, HSA and apoTf) were investigated by absorption and fluorescence spectroscopy. The binding constants were found to be (1 ? 20) ¡Á 10⁵ mol^-1¡¤L. By comparison, ¦Â-substituted 2 had stronger combining ability with albumin than that of ¦Á-substituted 1. The non-covalent conjugates (1-BSA, 2-BSA, 1-HSA, 1-apoTf and 1-FeTf) with the molar ratio of about 1 : 1 have also been prepared The photodynamic activities of two complexes and their bioconjugates against MCF-7 mammary tumor cells were examined The result shows that the photocytotoxicities of conjugates are higher than that of complexes 1 ? 2 and follows the order 1-BSA > 1-FeTf > 1-HSA, 1-apoTf > 2-BSA > 1>2.

Wuji Huaxue Xuebao 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, Computed Properties of 67914-60-7.

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

Zhao, Lihua published the artcileDesign, synthesis and antitumor activity of thalidomide derivatives, Category: piperazines, the publication is Zhongguo Yaowu Huaxue Zazhi (2008), 18(1), 16-22, database is CAplus.

The antitumor activity of thalidomide derivatives [i.e., 2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione derivatives] was studied. A method for the synthesis of the title compounds is reported here. According to the structure of thalidomide, starting from ¦Â-D-glucosamine hydrochloride, twenty compounds were designed and synthesized. Product structures were determined by NMR, IR, MS. The target compounds were evaluated for their anticancer activity. The survival of 4T1 cells was determined Compounds substituted by a 3,4,6-tri-O-acetyl glucopyranoside have better antitumor activity than thalidomide dose.

Zhongguo Yaowu Huaxue Zazhi 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 C2H4ClNO, Category: piperazines.

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

Liang, Shuang published the artcileSynthesis and antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substituted)-1-piperazinyl]-2-propanols, Category: piperazines, the publication is Zhongguo Yaowu Huaxue Zazhi (2004), 14(2), 71-75, database is CAplus.

The effect of the side chain in (4-substituted)-1-piperazinyl on the antifungal activity of fluconazole compounds was studied. Thirteen title compounds were synthesized and confirmed by the elementary anal., ¹H-NMR and IR spectra. The MICs of all the title compounds were determined by the method recommended by the National Committee for Clin. Laboratory Standards (NCCLS) using the RPMI1640 test medium. The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities. The activities of the eight compounds thus prepared were more than 4 times as high as that of fluconazole and equal to that of ketoconazole against Candida albicans in vitro. The lipid/water distribution coefficient and stereochem. have important influence on the antifungal activities of the title compounds

Zhongguo Yaowu Huaxue Zazhi 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

He, Qiuqin published the artcileSynthesis and antifungal activities of 1-(1H-1,2,4-triazol-1-y1)-2-(2,4-difluorophenyl)-3-[(4-substituted)-piperazin-1-y1]-2-propanol, Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Zhongguo Yaowu Huaxue Zazhi (2007), 17(1), 8-12, database is CAplus.

According to the structure of fluconazole, eleven target compounds were designed and synthesized. All of them were confirmed by H-NMR or IR spectra, resp. The MIC₈₀ of all the target compounds were determined by the method recommended by the national committee for clin. laboratory standards (NCCLS) using the RPMI 1640 test medium. Eleven target compounds were firstly reported. The results of the preliminary antifungal test showed that all the target compounds exhibited potent antifungal activities to a certain extent. Most of the target compounds showed higher antifungal activities than that of fluconazole. Especially, compound I showed strong antifungal activity with broad antifungal spectrum and was chosen for further study.

Zhongguo Yaowu Huaxue Zazhi 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

Wang, Chenxuan published the artcileInhibition of ¦¤-6 desaturase reduces fatty acid re-esterification in 3T3-L1 adipocytes independent of changes in n3-PUFA cellular content, Category: piperazines, the publication is Biochimica et Biophysica Acta, Molecular and Cell Biology of Lipids (2022), 1867(7), 159160, database is CAplus and MEDLINE.

¦¤-6 Desaturase (D6D) is a key enzyme in the synthesis of long-chain polyunsaturated fatty acids (LC-PUFA). Evidence suggests that reduced D6D activity not only disrupts LC-PUFA production, but also impacts whole body lipid handling and body weight; however, the mechanisms remain largely unexplored. Therefore, we investigated the effect of D6D inhibition on the regulation of lipid accumulation in 3T3-L1 adipocytes with and without changes in n-3 PUFA content. 3T3-L1 cells were treated with a D6D inhibitor (SC-26196) in the presence or absence of ¦Á-linolenic acid (ALA) throughout differentiation. We found that D6D inhibition blocked the conversion of ALA to eicosapentaenoic acid (EPA) and docosapentaenoic acid (DPAn-3) when ALA was supplemented, while no changes in n-3 PUFA content were observed in cells treated with the D6D inhibitor alone. D6D inhibited cells had reduced triacylglycerol (TAG) accumulation despite an EPA/DPA deficiency. In addition, analyses of cellular protein markers, as well as non-esterified fatty acids and glycerol release in medium, suggested an increase in lipolysis and a decrease in fatty acid re-esterification in D6D-inhibited cells, independent of n-3 PUFA changes. To provide further evidence, we treated cells with the D6D inhibitor in the presence or absence of EPA and compared them with ALA-treated cells. Although EPA further reduced TAG content, the reduced markers of fatty acid re-esterification were not affected by ALA or EPA. Collectively, this study provides new insight showing that D6D inhibition reduces TAG accumulation and fatty acid re-esterification in adipocytes independent of changes in n-3 PUFA cellular content.

Biochimica et Biophysica Acta, Molecular and Cell Biology of Lipids published new progress about 218136-59-5. 218136-59-5 belongs to piperazines, auxiliary class Metabolic Enzyme,D6D, name is 2,2-Diphenyl-5-(4-((pyridin-3-ylmethylene)amino)piperazin-1-yl)pentanenitrile, and the molecular formula is C13H16O2, Category: piperazines.

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

Schiaffella, Fausto published the artcileNovel ketoconazole analogues based on the replacement of 2,4-dichlorophenyl group with 1,4-benzothiazine moiety: Design, synthesis, and microbiological evaluation, Category: piperazines, the publication is Bioorganic & Medicinal Chemistry (2006), 14(15), 5196-5203, database is CAplus and MEDLINE.

As a part of a program to develop novel antifungal agents, new compounds which incorporate the 1,4-benzothiazine moiety into the structure of ketoconazole (KTZ) were prepared These compounds were computationally investigated to assess whether the 1,4-benzothiazine moiety was a suitable bioisosteric replacement for the 2,4-dichlorophenyl group of KTZ in order to obtain a more potent inhibition of CYP51 enzyme of Candida albicans. Results of preliminary microbiol. studies show that the racemic cis-7 analog has a good in vivo activity, comparable to that of KTZ, but the best activity was observed in the racemic trans-7 analog.

Bioorganic & 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, Category: piperazines.

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