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排序方式: 共有163条查询结果,搜索用时 431 毫秒
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Peng Cheng Linlin Yang Xiaodan Huang Xuejun Wang Maoqing Gong 《Archiv der Pharmazie》2020,353(4):1900350
Malaria, one of the most striking, re-emerging infectious diseases caused by the genus Plasmodium, places a huge burden on global healthcare systems. A major challenge in the control and eradication of malaria is the continuous emergence of increasingly widespread drug-resistant malaria, creating an urgent need to develop novel antimalarial agents. Chalcone derivatives are ubiquitous in nature and have become indispensable units in medicinal chemistry applications due to their diverse biological profiles. Many chalcone derivatives demonstrate potential in vitro and in vivo antimalarial activity, so chalcone could be a useful template for the development of novel antimalarial agents. This review covers the recent development of chalcone hybrids as antimalarial agents. The critical aspects of the design and structure–activity relationship of these compounds are also discussed. 相似文献
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目的:为进一步揭示红花Carthamus tinctorius L.药理活性的化学物质基础,开发其活性成分,我们对其进行了较为深入系统的化学成分研究。方法;经大孔树脂,硅胶和Sephadex LH-20反复柱层分得并通过波波谱分析鉴定了12个化合物。结果:它们分别为2,3,4,9-tetrahydro-1-methyl-1-H-pyrido[3,4-b]indole-3-carboxylicacid(Ⅰ);thymine-2-desoxyribofuranoside(Ⅱ);ethyl-α-D-lyxofuranoside(Ⅲ);kaempferol-3-O-rutinoside(Ⅳ);syringin(Ⅴ);quercetin-3-O-β-D-galactoside(Ⅵ);safflor yellow-A(Ⅶ);carthamin(Ⅷ)和阿魏酸,对羟基玻酸,胡萝卜苷,β-谷甾醇。结论:化合物Ⅰ,Ⅱ和Ⅲ为首次从该植物中分得。化合物Ⅶ对ADP诱导的大鼠血小板聚集有较好的抑制活性。 相似文献
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Chuan Xie Siyu Zhang Wei Zhang Chunxia Wu Can Yong Yuhao Sun Zhengxing Zeng Qian Zhang Zixin Huang Tian Chen Yuanyuan Zhang 《Chemical biology & drug design》2020,96(2):836-849
The issue of antibiotic resistance is becoming progressively serious these days, and the feasible solution to address it is to develop and discover novel antibiotics. The diterpene natural pleuromutilin is a prominent candidate for its special mode of action by inhibiting protein synthesis. In this study, a series of novel pleuromutilin derivatives with chalcone moiety was designed and synthesized, and their antibacterial activities were assessed in vitro. As suggested from the results, most of compounds exhibited potent activities against two methicillin‐resistant Staphylococcus aureus (MRSA) ATCC 33591 and 43300. The further modification of the chalcone structure, aza‐cyclic derivatives were afforded and then assessed, and potent activities against the tested strains were reported. The preliminary docking studies were conducted to explore the interactions between target molecules and binding site. 相似文献
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目的:研究查尔酮化合物B1、B2对过氧化氢(H2O2)诱导的PC12细胞凋亡的保护作用及其对Nrf2/ARE信号通路的影响。方法:建立H2O2诱导PC12细胞氧化损伤的模型,用MTT法检测化合物B1和B2的抗氧化活性及细胞毒性;用实时荧光定量PCR(real-time PCR)法检测其对转录相关因子Nrf2调控基因谷氨酰半胱氨酸合成酶催化亚单位(GCLC)、血红素氧合酶-1(HO-1)m RNA表达的影响;用Hoechst染色检测其对H2O2诱导的PC12细胞凋亡的抑制作用。结果:分别加了B1、B2的细胞孵育1 h后,B1、B2对H2O2诱导的PC12细胞氧化损伤无保护作用,而孵育24 h后,B1、B2均具有较好的保护作用,两者在浓度为10μmol/L时对细胞无毒性;B1对Nrf2下游GCLC、HO-1基因的表达无明显影响,而B2可明显激活GCLC、HO-1基因的表达,且明显抑制H2O2诱导的PC12细胞的凋亡。结论:B1、B2均对H2O2诱导的PC12细胞损伤具有较好的抗氧化保护作用,B2的作用机制可能是通过激活Nrf2/ARE抗氧化信号通路来实现,B1可能是通过其他机制起到抗氧化作用。 相似文献
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Viviana Cuartas Sara M. Robledo Iván D. Vélez María del Pilar Crespo Maximiliano Sortino Susana Zacchino Manuel Nogueras Justo Cobo Yulieth Upegui Tatiana Pineda Lina Yepes Braulio Insuasty 《Archiv der Pharmazie》2020,353(5):e1900351
A new series of N-substituted pyrazoline derivatives 6a–g , 7a–g , 8a–g , and 9a–g was synthetized by reaction of hydrazine derivatives and chalcone–thiazole hybrids bearing nitrogen mustard 5a–g . The chalcones 5a–g were obtained by Claisen–Schmidt condensation of thiazole-2-nitrogen mustard 3 and selected acetophenones 4a–g . These new compounds 6/7/8/9a–g were screened for their antifungal activity against Cryptococcus neoformans, with IC50 values of 3.9–7.8 µg/ml for the N-3,5-dichlorophenyl pyrazolines 9e – g . Interestingly, those compounds show low cytotoxic effects toward erythrocytes (RBC). In addition, N-acetyl ( 6a,b ) and N-formyl pyrazolines ( 7a , 7b , 7c , and 7g ) showed inhibitory activity against methicillin-susceptible Staphylococcus aureus, methicillin-resistant S. aureus, and vancomycin-intermediate S. aureus, with the most important minimum inhibitory concentration values ranging from 31.25 to 125 µg/ml. Regarding the antiprotozoal activity, thiazolyl-pyrazolines 9g , 8f , and 7c display high activity against Plasmodium falciparum, Leishmania (V) panamensis, and Trypanosoma cruzi, with EC50 values of 11.80, 6.46, and 4.98 μM, respectively, and with 7c being approximately 2.6-fold more potent than benznidazole with a selectivity index of 1.61 on U-937 human cells, showing promising potential as a novel antitrypanosomal agent. 相似文献
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The continuous emergency of drug-resistant cancers and the low specificity of anticancer agents have been the major challenges in the control and treatment of cancer, making an urgent need to develop novel anticancer agents with high efficacy. Chalcones, precursors of flavonoids and isoflavonoids, exhibit structural heterogeneity and can act on various drug targets. Chalcones which demonstrated potential in vitro and in vivo activity against both drug-susceptible and drug-resistant cancers, are useful templates for the development of novel anticancer agents. Hybridization of chalcone moiety with other anticancer pharmacophores could provide the hybrids which have the potential to overcome drug resistance and improve the specificity, so it represents a promising strategy to develop novel anticancer agents. This review emphasizes the development, the mechanisms of action as well as structure-activity relationships of chalcone hybrids with potential therapeutic application for many cancers in recent 10 years. 相似文献