- Synthetic method of 3-bromo-7-methoxyl quinoline
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The invention provides a synthetic method of 3-bromo-7-methoxyl quinoline. The synthetic method of 3-bromo-7-methoxyl quinoline comprises the following steps: 1) adding a solvent into 7-nitryl-1,2,3,4-tetrahydroquinoline, adding DDQ and stirring the mixture to react to obtain 7-nitryl quinoline, wherein the molar ratio of 7-nitryl-1,2,3,4-tetrahydroquinoline and DDQ is 1: (1-5); 2) adding the solvent into 7-nitryl quinoline, heating the mixture, adding N-bromo-succinimide to react to obtain 3-bromo-7-nitryl quinoline in an insulating manner; and 3) dissolving 3-bromo-7-nitryl quinoline in thesolvent, adding sodium methylate, and heating the mixture to stir and react to obtain 3-bromo-7-methoxyl quinoline. The synthetic method of 3-bromo-7-methoxyl quinoline is concise in synthetic route,reasonable in process selection, low in raw material cost, simple and easy, convenient to operate and post-treat, high in total yield and easy to amplify.
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Paragraph 0037; 0038; 0053; 0055
(2018/11/22)
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- Synthesis and antibacterial activity of novel ketolides with 11,12-quinoylalkyl side chains
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A series of quinoylalkyl side chains was designed and synthesized, followed by introduction into ketolides by coupling with building block 6 or 32. The corresponding targets 7a–n, 33b, and 33e were tested for their in vitro activities against a series of macrolide-sensitive and macrolide-resistant pathogens. Some of them showed a similar antibacterial spectrum and comparable activity to telithromycin. Among them, two C2-F ketolides, compounds 33b and 33e, displayed excellent activities against macrolide-sensitive and macrolide-resistant pathogens.
- Zhao, Zhe-hui,Zhang, Xiao-xi,Jin, Long-long,Yang, Shuang,Lei, Ping-sheng
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supporting information
p. 2358 - 2363
(2018/06/25)
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- NOVEL SUBSTITUTED BICYCLIC AROMATIC COMPOUNDS AS S-NITROSOGLUTATHIONE REDUCTASE INHIBITORS
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The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
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Page/Page column 98
(2012/06/30)
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- 17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS FOR THE TREATMENT OF HORMONE-RELATED DISEASES
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The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases.The invention further relates to suitable inhibitors and to a method for the production thereof.
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Page/Page column 12
(2010/08/18)
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- Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: Potent and selective nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases
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Human 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyzes the reduction of the weak estrogen estrone (E1) to the highly potent estradiol (E2). This reaction takes place in the target cell where the estrogenic effect is exerted via the estrogen receptor (ER). Estrogens, especially E2, are known to stimulate the proliferation of hormone-dependent diseases. 17β-HSD1 is overexpressed in many breast tumors. Thus, it is an attractive target for the treatment of these diseases. Ligand- and structure-based drug design led to the discovery of novel, selective, and potent inhibitors of 17β-HSD1. Phenyl-substituted bicyclic moieties were synthesized as mimics of the steroidal substrate. Computational methods were used to obtain insight into their interactions with the protein. Compound 5 turned out to be a highly potent inhibitor of 17β-HSD1 showing good selectivity (17β-HSD2, ERα and β), medium cell permeation, reasonable metabolic stability (rat hepatic microsomes), and little inhibition of hepatic CYP enzymes.
- Frotscher, Martin,Ziegler, Erika,Marchais-Oberwinkler, Sandrine,Kruchten, Patricia,Neugebauer, Alexander,Fetzer, Ludivine,Scherer, Christiane,Müller-Vieira, Ursula,Messinger, Josef,Thole, Hubert,Hartmann, Rolf W.
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p. 2158 - 2169
(2008/12/20)
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