528-48-3Relevant articles and documents
A synthesis method of fisetin
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Paragraph 0017; 0051; 0062-0065; 0066; 0077-0080; 0081- 0155, (2019/04/10)
The invention provides a method for synthesis of fisetin, solves the fisetin synthetic method only is suitable for the laboratory, and the product yield and content can't problem. The synthetic method comprises the following steps: 1) using 2 - butanone, benzyl chloride, 2, 4 - dihydroxy acetophenone and anhydrous K2 CO3 Generating on the protecting group of the intermediate product; 2) under the protection of nitrogen, in the alkaline environment, the intermediate product and protocatechuic aldehyde condensation reaction, generating 3 ', 4' - dihydroxy - 7 - [...]; 3) the 3 ', 4' - dihydroxy - 7 - [...] reduction generating 3 ', 4', 7 - three hydroxy chalcone; 4) the 3 ', 4', 7 - three hydroxy chalcone is placed on in the alkaline environment of hydroxy, then in toluene sulfonic acid catalysis of a cyclization reaction, generating fisetin. The synthesis method can be used for industrial production; the synthetic method is simple in operation, raw materials are easy, and the production cost is low, and the resulting intermediate product and finally the yield of the product, the higher the purity, has good prospects for development.
Profiling of flavonol derivatives for the development of antitrypanosomatidic drugs
Borsari, Chiara,Lucian, Rosaria,Pozzi, Cecilia,Poehner, Ina,Henrich, Stefan,Trande, Matteo,Cordeiro-Da-silva, Anabela,Santarem, Nuno,Baptista, Catarina,Tait, Annalisa,Di Pisa, Flavio,Iacono, Lucia Dello,Landi, Giacomo,Gul, Sheraz,Wolf, Markus,Kuzikov, Maria,Ellinger, Bernhard,Reinshagen, Jeanette,Witt, Gesa,Gribbon, Philip,Kohler, Manfred,Keminer, Oliver,Behrens, Birte,Costantino, Luca,Nevado, Paloma Tejera,Bifeld, Eugenia,Eick, Julia,Clos, Joachim,Torrado, Juan,Jiménez-Antón, María D.,Corral, María J.,Alunda, José Ma,Pellati, Federica,Wade, Rebecca C.,Ferrari, Stefania,Mangani, Stefano,Costi, Maria Paola
, p. 7598 - 7616 (2016/09/04)
Flavonoids represent a potential source of new antitrypanosomatidic leads. Starting from a library of natural products, we combined target-based screening on pteridine reductase 1 with phenotypic screening on Trypanosoma brucei for hit identification. Flavonols were identified as hits, and a library of 16 derivatives was synthesized. Twelve compounds showed EC50 values against T. brucei below 10 μM. Four X-ray crystal structures and docking studies explained the observed structure-activity relationships. Compound 2 (3,6-dihydroxy-2-(3-hydroxyphenyl)-4H-chromen-4-one) was selected for pharmacokinetic studies. Encapsulation of compound 2 in PLGA nanoparticles or cyclodextrins resulted in lower in vitro toxicity when compared to the free compound. Combination studies with methotrexate revealed that compound 13 (3-hydroxy-6-methoxy-2-(4-methoxyphenyl)-4H-chromen-4-one) has the highest synergistic effect at concentration of 1.3 μM, 11.7-fold dose reduction index and no toxicity toward host cells. Our results provide the basis for further chemical modifications aimed at identifying novel antitrypanosomatidic agents showing higher potency toward PTR1 and increased metabolic stability.
Isolation and synthesis of flavonols and comparison of their antioxidant activity
Hasan, Aurangzeb,Sadiq,Abbas,Mughal,Khan, Khalid M.,Ali, Muhammad
experimental part, p. 995 - 1003 (2010/09/05)
Phytochemical investigation of the leaves of Astragalus beckari yielded four flavonol aglycones, namely kaempferol, quercetin, 5-deoxy kaempferol and fisitin. These isolated compounds were then synthesised in the laboratory using the Algar-Flyn-Oyamad reaction. Antioxidant activity of both the isolated and synthesised flavonoids was compared using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay method. The isolated flavonoids were found to be more active.