- Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria
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Infections due to rapidly growing mycobacteria (RGM), and in particular the RGM species Mycobacterium abscessus (Mab), are very difficult to treat and reports on novel therapeutic options are scarce. A hallmark of all pathogenic RGM species is their resis
- Combrink, Keith D.,Ramos, Andrea Ramirez,Spring, Stephanie,Schmidl, Sebastian,Elizondo, Kira,Morin, Petronilo,De Jesus, Bryant,Maurer, Florian P.
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Read Online
- Quinazoline derivatives preparation method and use thereof
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The invention discloses a quinazoline derivative shown in formula (I) which is described in the specification and a salt thereof. In the formula, Z represents -NH- and -O-, R1 and R2 represent C1-3 alkoxy groups or hydrogen, R3 is selected from the group consisting of 4-fluoro-, 4-chloro-, 2-chloro-, 4-bromo-, 2, 4-dichloro-, 4-methyl, 4-methoxy, hydrogen, 4-trifluoromethyl and 2,4-dimethoxy. The invention relates to a preparation method and application of the compound shown in the formula (I) and the salt thereof. The compound or the salt thereof has strong inhibitory activity on colorectal cancer cell strains HCT-116, human lung cancer cell strains A549 and breast cancer cell strains MCF-7. The compound has wide spectrum antitumor activity and can be used as a drug or lead compound for treatment of diseases like tumors and cancers.
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- Synthesis and biological evaluation of isoxazolyl-sulfonamides: A non-cytotoxic scaffold active against Trypanosoma cruzi, Leishmania amazonensis and Herpes Simplex Virus
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In this study we report the synthesis, characterization, biological evaluation, and druglikeness assessment of a series of 20 novel isoxazolyl-sulfonamides, obtained by a four-step synthetic route. The compounds had their activity against Trypanosoma cruz
- da Rosa, Rafael,Zimmermann, Lara Almida,de Moraes, Milene H?ehr,Schneider, Naira Fernanda Zanchett,Schappo, Alice Duarte,Sim?es, Claudia Maria de Oliveira,Steindel, Mario,Schenkel, Eloir Paulo,Bernardes, Lílian Sibelle Campos
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p. 3381 - 3384
(2018/09/11)
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- Ferrocene derivatives, preparation method and use thereof
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The invention discloses ferrocene derivatives as shown in a formula I in the specification and salts thereof, wherein Z is O or NH; R is selected from hydrogen, fluorine, chlorine, bromine, methyl, methoxyl and trifluoromethyl; n is an integer ranging fro
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Paragraph 0076; 0077; 0084; 0085; 0088
(2018/10/11)
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- Quinazoline derivatives and their use
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The present invention provides a quinazoline compound shown in formula (I), or pharmaceutically acceptable salt thereof. R1, R2 and R7 are independently and respectively selected from hydrogen, C1-6 alkyl, C1-6 alkoxy, halogenate C1-6 alkyl, halogenate C1
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- Thiophene [2, 3 - d] pyrimidine derivatives, their preparation and use thereof
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The invention provides a thiophene [2, 3-d] pyrimidine derivative containing isoxazole heterocycle shown by formula (I) or a pharmaceutically accepted salt thereof, wherein R1 and R2 are respectively selected from hydrogen, C1-6 alkyl, C1-6 alkoxy, haloge
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- THIOPHENE [2, 3-D]PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD AND USE THEREOF
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This invention provides thieno[2,3-d]pyrimidine derivatives containing isoxazole heterocycle represented by formula (I), or pharmaceutically acceptable salts thereof Wherein: R1 and R2 may be the same or different and is independentl
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- QUINAZOLINE DERIVATIVE AND APPLICATION THEREOF
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This invention provides a class of quinazoline compounds, as represented by formula (I), and their pharmaceutically acceptable salts, wherein: each of R1 and R2 independently, is selected from H, C1-C6 alkoxy, h
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- QUINAZOLINE DERIVATIVE AND APPLICATION THEREOF
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This invention provides a class of quinazoline compounds, as represented by formula (I), and their pharmaceutically acceptable salts, wherein: each of R1 and R2 independently, is selected from H, C1-C6 alkoxy, h
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- Design, synthesis and antibacterial activity of novel N-formylhydroxylamine derivatives as PDF inhibitors
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A new series of N-formylhydroxylamines 11a-i have been synthesized through a multi-step protocol starting from diethyl malonate. These compounds have been structurally characterized by IR, 1H NMR and HRMS. All the synthesized compounds 11a-i have been screened for antibacterial activities. All the compounds are found to exhibit potent in vitro inhibitory activity against Staphylococcus aureus and relatively weak antibacterial activity against Klebsiella pneumoniae.
- Yin,Jia,Zhao,Xu,Tang,Wang
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experimental part
p. 695 - 703
(2011/07/29)
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- Synthesis and preliminary antibacterial evaluation of 2-butyl succinate-based hydroxamate derivatives containing isoxazole rings
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Two series of novel 2-butyl succinate-based Hydroxamate derivatives containing isoxazole rings were synthesized, characterized and evaluated for antibacterial activity. The synthesized compounds were found to exhibit weak to moderate inhibitory activity against Staphytlococcus aureu and Klebsiellar pneumonia in vitro. All the compounds synthesized were found to be more effective against Klebsiellar pneumonia compared to Staphytlococcus aureu.
- Zhang, Datong,Jia, Jiong,Meng, Lijuan,Xu, Weiren,Tang, Lida,Wang, Jianwu
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p. 831 - 842
(2012/01/04)
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- Design, synthesis, and herbicidal activities of novel 2-cyanoacrylates containing isoxazole moieties
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A series of novel 2-cyanoacrylates containing an isoxazole moiety were designed and synthesized. Their structures were characterized by 1H NMR and elemental analysis (or high-resolution mass spectrometry). Their herbicidal activities against four species were evaluated, and the results indicated that some of the title compounds showed excellent herbicidal activities against rape and amaranth pigweed in postemergence treatment even at a dose of 75 g/ha.
- Liu, Yuxiu,Cui, Zhipeng,Liu, Bin,Cai, Baoli,Li, Yonghong,Wang, Qingmin
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p. 2685 - 2689
(2011/07/07)
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- Methods of Using IGFIR and ABL Kinase Modulators
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The invention provides methods of treating cancer with a compound which inhibits kinases, more specifically IGF1R and Abl, in combination with treatments(s) selected from surgery, radiation, monoclonal antibody, bone marrow or peripheral blood stem cell t
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- GLYCYRRHETINIC ACID-30-AMIDE DERIVATIVES AND THE USES THEREOF
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The present invention relates to the field of a medicine for treating diseases associated with inflammation, immunity or infection, and in particular, to glycyrrhetinic acid-30-amide derivatives of general formula I and their preparation, and a pharmaceutical composition containing the same. Said derivatives and composition exhibit anti -inflammatory, analgesic, anti-allergic, cough-preventing, liver-protecting and anti-viral properties, wherein each group is as defined in the description.
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Page/Page column 11
(2008/12/06)
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- Pyrimidine Derivatives As Kinase Modulators and Method of Use
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The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. The invention provides compounds for modulating protein kinase enz
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Page/Page column 144
(2008/12/08)
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- Regioselective syntheses of 3-aminomethyl-5-substituted isoxazoles: A facile and chemoselective reduction of azide to amino by sodium borohydride using 1,3-propanedithiol as a catalyst
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A series of isoxazole azides were reduced selectively to isoxazole amines in quantitative yield by sodium borohydride using 1,3-propanedithiol as a catalyst.
- Pei,Wickhan
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p. 7509 - 7512
(2007/10/02)
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