- 8-Hydroxyquinolin-2(1H)-one analogues as potential β2-agonists: Design, synthesis and activity study
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β2-Agonists that bind to plasmalemmal β2-adrenoceptors causing cAMP accumulation are widely used as bronchodilators in chronic respiratory diseases. Here, we designed and synthesized a group of 8-hydroxyquinolin-2(1H)-one analogues and studied their β2-agonistic activities with a cellular cAMP assay. Compounds B05 and C08 were identified as potent (EC50 2-agonists among the compounds tested. They behaved as partial β2-agonists in non-overexpressed HEK293 cells, and possessed rapid smooth muscle relaxant actions and long duration of action in isolated guinea pig tracheal strip preparations. In summary, B05 and C08 are β2-agonists with potential applicability in chronic respiratory diseases.
- Xing, Gang,Zhi, Zhengxing,Yi, Ce,Zou, Jitian,Jing, Xuefeng,Yiu-Ho Woo, Anthony,Lin, Bin,Pan, Li,Zhang, Yuyang,Cheng, Maosheng
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- Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β2-adrenoceptor agonists
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A series of β2-adrenoceptor agonists with an 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one moiety is presented. The stimulatory effects of the compounds on human β2-adrenoceptor and β1-adrenoceptor were characterized by a cell-based assay. Their smooth muscle relaxant activities were tested on isolated guinea pig trachea. Most of the compounds were found to be potent and selective agonists of the β2-adrenoceptor. One of the compounds, (R)-18c, possessed a strong β2-adrenoceptor agonistic effect with an EC50 value of 24 pM. It produced a full and potent airway smooth muscle relaxant effect same as olodaterol. Its onset of action was 3.5 min and its duration of action was more than 12 h in an in vitro guinea pig trachea model of bronchodilation. These results suggest that (R)-18c is a potential candidate for long-acting β2-AR agonists.
- Yi, Ce,Xing, Gang,Wang, Siqi,Li, Xiaoran,Liu, Yichuang,Li, Jinyan,Lin, Bin,Woo, Anthony Yiu-Ho,Zhang, Yuyang,Pan, Li,Cheng, Maosheng
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- Transition-metal-free Intramolecular C-H amination of sulfamate esters and: N -alkylsulfamides
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The transition-metal-free intramolecular C-H amination of sulfamate esters using iodine oxidants, tert-butyl hypoiodite (t-BuOI) and N-iodosuccinimide (NIS) is reported. A method using NIS was also successfully applied to the oxidative cyclization of N-alkylsulfamides.
- Kiyokawa, Kensuke,Nakamura, Shogo,Jou, Keisuke,Iwaida, Kohji,Minakata, Satoshi
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supporting information
p. 11782 - 11785
(2019/10/02)
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- Catalytic sp3C-CN Bond Cleavage: Ni-Mediated Phosphorylation of Alkylnitriles
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A direct phosphorylation of the sp3C-CN bond catalyzed by a nickel catalyst is disclosed. A wide range of primary nitriles readily coupled with secondary phosphine oxides to produce the corresponding phosphorylated products in high yields. As a key step, this new method was applied to the synthesis of anticancer drug Combretastatin-A4, significantly shortening its synthetic path.
- Zhang, Ji-Shu,Chen, Tieqiao,Zhou, Yongbo,Yin, Shuang-Feng,Han, Li-Biao
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supporting information
p. 6746 - 6749
(2018/10/25)
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- Method for synthesizing substituted acrylonitrile with one-pot process
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The invention provides a method for synthesizing substituted acrylonitrile with a one-pot process. Beta-aryl substituted acrylonitrile is prepared from 0.01-1.0 mol of aryl substituted methanol or heterocycle substituted methanol as a raw material and a solvent adopting acetonitrile with the concentration of 0.2-2.0 mol/L under the alkaline action. In the oxygen atmosphere, a semiconductor photocatalyst is added, the mixture reacts under assistance of light illumination, and the reaction speed and the yield can be greatly increased. Raw materials for a reaction are easy to obtain, the method is simple and convenient, and the product has important application value.
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Paragraph 0022; 0023; 0024; 0037; 0038; 0039; 0040
(2017/06/02)
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- 18F-LABELLED ALDEHYDE COMPOSITIONS FOR RADIOFLUORINATION
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The present invention relates to improved 18F-labelled aldehyde compositions, wherein impurities which affect imaging in vivo are identified and suppressed. Also provided are methods of preparation of radiofluorinated biological targeting molec
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Page/Page column 36
(2014/06/23)
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- Oxadiazole and oxadiazoline derivatives
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There are described new compounds of formula STR1 in which E is selected from the group consisting of residues of formula STR2 in which R" is selected from the group consisting of amino, vinyl, allyl, ethynyl, C1 -C5 alkyl, C1 -C5 alkoxy, or C1 -C5 alkylthio or a C1 -C5 alkyl group susbstituted by at least one halogen atom; and hydrogen; in which R1 and R2 are each selected from the group consisting of hydrogen, halogen, methyl and ethyl; and R' is selected from substituted phenyl when R" is other than hydrogen, and phenyl, thienyl and substituted phenyl and thienyl when R" is hydrogen. The compounds are useful in the control of parasites. Certain of the compounds have antimicrobial properties.
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