1577-03-3Relevant articles and documents
Design, synthesis and neuraminidase inhibitory activity of N-(5-benzyl-4-(tert-butyl)thiazol-2-yl)benzamides
Wu, Zhilin,Peng, Junmei,Hu, Aixi,Ye, Jiao,Li, Guoxi
, p. 356 - 368 (2016)
A series of N-(5-benzyl-4-(tert-butyl)thiazol-2-yl)benzamides were synthesized and the structures were characterized by 1H NMR, MS and elemental analyses. The crystal structures of compounds F5 and F16 were determined by single-crystal X-ray diffraction. The neuraminidase inhibitory activities of compounds F1-F32 were evaluated in vitro at the concentration of 40 μg/mL. The results indicated that compounds F8, F26 and F32 exhibited most potent inhibitory activity against NA. Molecular docking was performed by LeDock to further explain the structure-activity relationship of compound F26. The docking modeling showed that compound F26 was in good combination with oseltamivir binding sites of NA and could be a potential NA inhibitor agent.
Industrial synthesis method of tebuconazole intermediate alpha
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Paragraph 0039-0047, (2019/04/26)
The invention provides an industrial synthesis method of tebuconazole intermediate alpha. The method includes the following steps that an organic solvent, alkali, pinacone and an antioxidant are addedinto a reaction vessel, p-chlorobenzaldehyde is added i
2-Oxindole Acts as a Synthon of 2-Aminobenzoyl Anion in the K2CO3-Catalyzed Reaction with Enones: Preparation of 1,4-Diketones Bearing an Amino Group and Their Further Transformations
Miao, Chun-Bao,Zeng, Yu-Mei,Shi, Tong,Liu, Rui,Wei, Peng-Fei,Sun, Xiao-Qiang,Yang, Hai-Tao
, p. 43 - 50 (2016/01/15)
A convenient approach for the synthesis of 1,4-diketones bearing an amino group has been developed through the K2CO3-catalyzed reaction of 2-oxindoles with enones with the assistance of atmospheric O2 via sequential Michael addition-oxidation-ring-cleavage process. The further intramolecular reaction leads to the formation of benzoazepinone, quinoline, and 3-oxindole derivatives.
ALLOSTERIC INHIBITORS OF ATYPICAL PROTEIN KINASES C
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Paragraph 0086; 0108; 0121, (2015/06/08)
The invention provides specific small molecule compounds that allosterically regulate the activity of atypical protein kinase C, their use as a medicament, and their use in the treatment and prevention of allergic, inflammatory and autoimmune disorders, cancer, hyperproliferation, sepsis, viral and protozoan infections, dementing diseases, metabolic, sclerotic and osteoporotic disorders.
Discovery and optimization of 1,3,5-trisubstituted pyrazolines as potent and highly selective allosteric inhibitors of protein kinase C-χ
Abdel-Halim, Mohammad,Diesel, Britta,Kiemer, Alexandra K.,Abadi, Ashraf H.,Hartmann, Rolf W.,Engel, Matthias
supporting information, p. 6513 - 6530 (2014/10/15)
There is increasing evidence that the atypical protein kinase C, PKCχ, might be a therapeutic target in pulmonary and hepatic inflammatory diseases. However, targeting the highly conserved ATP-binding pocket in the catalytic domain held little promise to
Processes for preparing beta-hydroxy-ketones and alpha,beta-unsaturated ketones
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Page 16, (2008/06/13)
Processes for producing β-hydroxy-ketones and α,β-unsaturated ketones are disclosed which comprise the crossed condensation of an aldehyde with a ketone in the presence of a hydroxide or alkoxide of alkali metal or an alkaline earth metal as catalyst. The products of the process, β-hydroxy-ketones and α,β-unsaturated ketones, are useful for the preparation of many commercially important products in the chemical process industries including solvents, drug intermediates, flavors and fragrances, other specialty chemical intermediates.
Fungicidal compounds
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, (2008/06/13)
Triazoles of formula: STR1 wherein R1 is alkenyl, alkynyl or optionally substituted aralkyl; Y is =N--, R2 is cycloalkyl, alkyl or haloalkyl, and R3 is H, methyl or alkenyl, or esters, ethers, salts and metal complexes thereof. The triazoles have fungicidal and plant growth regulating activity.