190323-49-0Relevant articles and documents
Synthesis and antibacterial activity of novel myricetin derivatives containing sulfonylpiperazine
He, Jun,Tang, Xue-Mei,Liu, Ting-Ting,Peng, Feng,Zhou, Qing,Liu, Li-Wei,He, Ming,Xue, Wei
, p. 1021 - 1027 (2021)
Myricetin derivatives containing sulfonylpiperazine were synthesized and their structures were confirmed by NMR and HRMS. The antibacterial activity results indicated that some compounds showed good antibacterial activity against Xanthomonas oryzaepv. ory
Design, synthesis, and antibacterial activity of novel myricetin derivatives containing sulfonate
Su, Shijun,Zhou, Qing,Tang, Xuemei,Peng, Feng,Liu, Tingting,Liu, Liwei,Xie, Chengwei,He, Ming,Xue, Wei
, p. 345 - 356 (2021)
A series of myricetin derivatives containing sulfonate groups were designed and synthesized. Preliminary antibacterial activity showed that most of the target compounds exhibited significant biological activities against Xanthomonas axonopodis pv. Citri (Xac), Ralstonia solanacearum (Rs), and Xanthomonas oryzae pv. Oryzae (Xoo). In particular, the EC50 value of compound 3e was 13.76?μg/cm3 against Xac, which was better than commercial reagents bismerthiazol (50.32?μg/cm3) and thiodiazole copper. (83.27?μg/cm3), and the EC50 value of compound 3j was 11.92?μg/cm3 against Xoo in vitro, The result was better than that of bismerthiazol (72.08?μg/cm3) and thiodiazole copper (99.26?μg/cm3). Compound 3j displayed the better in vivo activity against rice bacterial leaf blight than bismerthiazol and thiodiazole copper. Meanwhile, the antibacterial mechanism of compounds 3e and 3j was studied by scanning electron microscope (SEM). These results suggested that myricetin derivatives containing sulfonate can be considered as a new antibacterial reagents. Graphic abstract: [Figure not available: see fulltext.]
Design and synthesis of the 4H-chromenone derivatives against psoriasis
Du, Jun Cheng,Han, Xu,Liu, Xin Hua,Yan, Yaoyao,Zhang, Famin,Zhu, Rende
, (2022/02/03)
On basis of Quercetin moiety, two series of 20 new compounds were designed and synthesized accordingly in this study, and their anti-inflammatory activities in vitro and in vivo were evaluated. At last, compound 8A2: 3- (1- (2- (4- (5-bromo-2-chlorobenzoyl) piperazin-1-yl) ethyl)-1H-1,2,3-triazol-4-yl) methoxy)-5,7-dimethoxy-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one with low toxicity was found the best one for inhibiting of NO. Meanwhile, this compound could significantly inhibit the expression of IL-6 (Interleukin-6), TNF-α (Tumor necrosis factor-α) and IL-17 (Interleukin-17), and also significantly down-regulate IL-17 mRNA psoriasis model in vitro. Further studies were performed to establish mouse psoriasis model induced by Imiquimod (IMQ), and the preliminary mechanism indicated that compound 8A2 may alleviate mouse psoriasis through obstructed the JAK1/2-STAT1/3 pathway. This study should be provide a basis for further study of effective treatment of psoriasis.
Pharmacokinetics and Metabolites of 12 Bioactive Polymethoxyflavones in Rat Plasma
Chen, Hongping,Ding, Haiyan,Hu, Yuan,Li, Dan,Liu, Youping,You, Qiang
, p. 12705 - 12716 (2021/11/17)
Polymethoxyflavones (PMFs) are a subgroup of flavonoids possessing various health benefits. 3,5,7,4′-Tetramethoxyflavone (1), 5,6,7,4′-tetramethylflavone (2), 3,7,3′,4′-tetramethoxyflavone (3), 5,7,3′,4′-tetramethoxyflavone (4), 5-hydroxy-3,7,2′,4′-tetramethoxyflavone (5), 3,5,7,2′,4′-pentamethoxyflavone (6), 5-hydroxy-3,7,3′,4′-tetramethoxyflavone (7), 3-hydroxy-5,7,3′,4′-tetramethylflavone (8), 3,5,7,3′,4′-pentamethoxyflavone (9), 5-hydroxy-3,7,3′,4′,5′-pentamethoxyflavone (10), 3-hydroxy-5,7,3′,4′,5′-pentamethoxyflavone (11), and 3,5,7,3′,4′,5′-hexamethoxylflavone (12) were 12 bioactive and available PMFs. The aim of this study was to investigate the pharmacokinetic, metabolite, and antitumor activities as well as the structure-pharmacokinetic-antitumor activity relationships of these 12 PMFs to facilitate further studies of their medicinal potentials. The cytotoxicity of PMFs with a hydroxy group toward HeLa, A549, HepG2, and HCT116 cancer cell lines was generally significantly more potent than that of PMFs without a hydroxy group. Compounds 5, 7, 8, 10, and 11 were all undetectable in rat plasma, while compounds 1-4, 6, 9, and 12 were detectable. Both the number and position of hydroxy and methoxy groups played an important role in modulating PMF pharmacokinetics and metabolites.
