69397-93-9Relevant articles and documents
Synthesis and fungicidal activity of novel imidazo[4, 5-b]pyridine derivatives
Wu, Daoxin,Liu, Minhua,Li, Zhong,Dang, Mingming,Liu, Xingping,Li, Jianming,Huang, Lu,Ren, Yeguo,Zhang, Zai,Liu, Weidong,Liu, Aiping
, p. 8 - 14 (2019/05/21)
A series of novel imidazo[4,5-b]pyridine derivatives were synthesized and their structures were characterized by NMR spectroscopy, mass spectrometry and elemental analysis. The results of bioassays showed that some compounds exhibit good fungicidal activity against Puccinia polysora In particular, compound 7b showed an EC50 value of 4.00 mg/L, which was comparable with that of tebuconazole. Besides, preliminary structure-activity relationship was discussed.
Benzimidazole compound and application thereof
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Paragraph 0202; 0204; 0205, (2019/01/07)
The invention relates to a benzimidazole compound and an application thereof. The structure of the benzimidazole compound is shown as a formula I, and the compound is used as a focal adhesion kinase inhibitor and shows relatively good focal adhesion kinase (FAK) inhibition activity. Meanwhile, the benzimidazole compound has stronger medicine effect and better pharmacokinetic property and/or toxicological characteristics, such as good brain/plasma ratio, good bioavailability, good metabolic stability, and reduced inhibition to respiratory action of mitochondria. The benzimidazole compound has agood clinical application prospect.
A facile base-mediated synthesis of N-alkoxy-substituted benzimidazoles
Ansari, Nurul H.,Jordan, Arica L.,S?derberg, Bj?rn C.G.
supporting information, p. 4811 - 4821 (2017/07/17)
Base mediated cyclization of enamines derived from condensation of 2-nitroanilines with α-branched aldehydes, in the presence of an electrophile, affords N-alkoxy-substituted benzimidazoles with or without an oxygenate side chain in the 2-position.
A photocleavable masked nuclear-receptor ligand enables temporal control of C.elegans development
Judkins, Joshua C.,Mahanti, Parag,Hoffman, Jacob B.,Yim, Isaiah,Antebi, Adam,Schroeder, Frank C.
supporting information, p. 2110 - 2113 (2014/03/21)
The development and lifespan of C.elegans are controlled by the nuclear hormone receptor DAF-12, an important model for the vertebrate vitaminD and liverX receptors. As with its mammalian homologues, DAF-12 function is regulated by bile acid-like steroidal ligands; however, tools for investigating their biosynthesis and function invivo are lacking. A flexible synthesis for DAF-12 ligands and masked ligand derivatives that enable precise temporal control of DAF-12 function was developed. For ligand masking, photocleavable amides of 5-methoxy-N-methyl-2-nitroaniline (MMNA) were introduced. MMNA-masked ligands are bioavailable and after incorporation into the worm, brief UV irradiation can be used to trigger the expression of DAF-12 target genes and initiate development from dauer larvae into adults. The invivo release of DAF-12 ligands and other small-molecule signals by using photocleavable MMNA-masked ligands will enable functional studies with precise spatial and temporal resolution. Copyright
Luminescent bimetallic lanthanide bioprobes for cellular imaging with excitation in the visible-light range
Deiters, Emmanuel,Song, Bo,Chauvin, Anne-Sophie,Vandevyver, Caroline D. B.,Gumy, Frederic,Buenzli, Jean-Claude G.
experimental part, p. 885 - 900 (2009/07/01)
A series of homoditopic ligands H2LCX (X=4-6) has been designed to self-assemble with lanthanide ions (LnIII), resulting in neutral bimetallic helicates of overall composition [Ln 2(LCX)3] with the aim of testing the influence of substituents on the photophysical properties, particularly the excitation wavelength. The complex species are thermodynamically stable in water (logβ23 in the range 26-28 at pH 7.4) and display a metal-ion environment with pseudo-D3 symmetry and devoid of coordinated water molecules. The emission of EuIII, TbIII and Yb III is sensitised to various extents, depending on the properties of the ligand donor levels. The best helicate is [Eu2(L C5)3] with excitation maxima at 350 and 365 nm and a quantum yield of 9%. The viability of cervix cancer HeLa cells is unaffected when incubated with up to 500 μm of the chelate during 24 h. The helicate permeates into the cells by endocytosis and locates into lysosomes, which co-localise with the endoplasmatic reticulum, as demonstrated by counterstaining experiments. The relatively long excitation wavelength allows easy recording of bright luminescent images on a confocal microscope (μcxc = 405 nm). The new lanthanide bioprobe remains undissociated in the cell medium, and is amenable to facile derivatisation. Examination of data for seven Eu III and TbIII bimetallic helicates point to shortcomings in the phenomenological rules of thumb between the energy gap ΔE( 3ππ*-5DJ) and the sensitisation efficiency of the ligands.
Novel Enantiomeric Pure Beta Agonists, Manufacturing and Use as a Medicament Thereof
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Page/Page column 10, (2008/06/13)
The present invention relates to enantiomerically pure compounds of formula 1 wherein the groups m, n, B, X, R1, m and Ym- may have the meanings given in the claims and specification, methods for preparing them and their use as pharmaceutical compositions, particularly as pharmaceutical compositions for the treatment of respiratory complaints.
INTERMEDIATE OF 6-SUBSTITUTED-1-METHYL-1-H-BENZIMIDAZOLE DERIVATIVE AND METHOD FOR PRODUCING SAME
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, (2008/06/13)
[Subject] The object of the present invention is to provide new intermediates (IIa) and (III) of the 6-substituted-1-methyl-1-H-benzimidazol derivatives (I) which are publicly known pharmaceutically active ingredients, and a preparation procedure suitable
Benzimidazole- and benzothiazole-quinones: Excellent substrates for NAD(P)H:quinone oxidoreductase 1
Newsome, Jeffery J.,Colucci, Marie A.,Hassani, Mary,Beall, Howard D.,Moody, Christopher J.
, p. 3665 - 3673 (2008/09/21)
A series of benzimidazole- and benzothiazole-quinones has been synthesized. The ability of these heterocyclic quinones to act as substrates for recombinant human NAD(P)H:quinone oxidoreductase (NQO1), a two-electron reductase upregulated in tumour cells,
Medicament Combinations for the Treatment of Respiratory Diseases
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Page/Page column 36, (2010/11/28)
The present invention relates to new medicament combinations which contain in addition to one or more, preferably one compound of general formula 1 wherein A, B, R1, X, n and m may have the meanings given in the claims and in the specification, at least one other active substance 2, processes for preparing them and their use as pharmaceutical compositions.
INTERMEDIATE OF 6-SUBSTITUTED-1-METHYL-1-H-BENZIMIDAZOLE DERIVATIVE AND METHOD FOR PRODUCING SAME
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Page/Page column 47, (2008/06/13)
Disclosed are novel production intermediates (IIa) and (III) of a 6-substituted-1-methyl-1-H-benzimidazole derivative (I) as a publicly-known pharmaceutically active ingredient. Also disclosed is a production method suitable for mass synthesis of N-(5-sub