共查询到20条相似文献,搜索用时 125 毫秒
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《Arabian Journal of Chemistry》2022,15(5):103756
Heterocyclic compounds occupy an important position in chemistry because of their wide range of uses in drug design, photochemistry, agrochemicals, and other fields. Indole and indazole scaffolds are available from natural and synthetic sources, and molecules containing these scaffolds have been shown to have various biological effects, including anti-inflammatory, antibacterial, antiviral, antifungal, analgesic, anticancer, antioxidant, anticonvulsant, antidepressant, and antihypertensive activities. Indole and indazole molecules bind to receptors with high affinity, and thus are useful for the study of bioactive compounds involved in multiple pathways. In this review, we highlight the antihypertensive activity and the mechanisms of action of indole and indazole derivatives. In addition, structure–activity relationship studies of the antihypertensive effect are presented. 相似文献
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Karen Rodríguez-Villar Lilin Ypez-Mulia Miguel Corts-Gines Jacobo David Aguilera-Perdomo Edgar A. Quintana-Salazar Kevin Samael Olascoaga Del Angel Francisco Corts-Benítez Juan Francisco Palacios-Espinosa Olivia Soria-Arteche Jaime Prez-Villanueva 《Molecules (Basel, Switzerland)》2021,26(8)
Indazole is an important scaffold in medicinal chemistry. At present, the progress on synthetic methodologies has allowed the preparation of several new indazole derivatives with interesting pharmacological properties. Particularly, the antiprotozoal activity of indazole derivatives have been recently reported. Herein, a series of 22 indazole derivatives was synthesized and studied as antiprotozoals. The 2-phenyl-2H-indazole scaffold was accessed by a one-pot procedure, which includes a combination of ultrasound synthesis under neat conditions as well as Cadogan’s cyclization. Moreover, some compounds were derivatized to have an appropriate set to provide structure-activity relationships (SAR) information. Whereas the antiprotozoal activity of six of these compounds against E. histolytica, G. intestinalis, and T. vaginalis had been previously reported, the activity of the additional 16 compounds was evaluated against these same protozoa. The biological assays revealed structural features that favor the antiprotozoal activity against the three protozoans tested, e.g., electron withdrawing groups at the 2-phenyl ring. It is important to mention that the indazole derivatives possess strong antiprotozoal activity and are also characterized by a continuous SAR. 相似文献
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丹皮酚,即2-羟基-4-甲氧基苯乙酮,为一种天然酚类化合物,分离于毛莨科植物牡丹(Paeonia suffruticosa)的根皮和萝藦科植物徐长卿(Cynanchum paniculatum)的全株。由于丹皮酚特有的酚酮结构骨架,现代生物科学研究表明其具有广泛的生物活性。本文概述了丹皮酚的提取与合成及其生物活性,重点介绍了丹皮酚类衍生物及其生物活性。丹皮酚农用生物活性广谱,可作为开发新农药的先导结构。将丹皮酚研发成高效低风险小分子绿色农药符合社会发展需求,此方面研究值得重点关注。这对促进我国的新农药创制、农作物病虫害防治及提升现代农业的高科技含量均有积极的科学和实际意义。 相似文献
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低氧诱导因子l(HIF-1)与肿瘤细胞的生长、侵袭和耐药密切相关,在肿瘤细胞内HIF-1高度表达,因此新型的HIF-1抑制剂可作为潜在的抗肿瘤药物。 本文合成了9个1,3-取代吲唑衍生物。 通过蛋白质印迹(Western Blot)法及实时定量荧光PCR(Real time-PCR)等方法检测了其对HIF-1及其靶基因血管内皮生长因子(VEGF)表达水平的影响,并以3-(5'-羟甲基-2'-呋喃基)-1-苯甲基吲唑(YC-1)为阳性对照药物初步评价了其体外抗肝癌细胞增殖的生物活性。 实验发现化合物7b可显著抑制HIF-1及其下游靶基因VEGF的表达,且体外抗肝癌增殖生物活性优于YC-1,半抑制浓度(IC50)值为10.37 μmol/L。 研究结果表明,3-(5'-羟甲基-2'-呋喃)-1-(1″-对甲苯磺酰基)吲唑具有靶向抑制HIF及良好的抗肝癌活性作用。 相似文献
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Suzuki Y Oishi S Takei Y Yasue M Misu R Naoe S Hou Z Kure T Nakanishi I Ohno H Hirasawa A Tsujimoto G Fujii N 《Organic & biomolecular chemistry》2012,10(25):4907-4915
Two classes of fused nitrogen heterocycles were designed as CK2 inhibitor candidates on the basis of previous structure-activity relationship (SAR) studies. Various dipyrrolo[3,2-b:2',3'-e]pyridine and benzo[g]indazole derivatives were prepared using transition-metal-catalysed cascade and/or multicomponent reactions. Biological evaluation of these candidates revealed that benzo[g]indazole is a promising scaffold for potent CK2 inhibitors. The inhibitory activities on cell proliferation of these potent CK2 inhibitors are also presented. 相似文献
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Rodríguez J Olea-Azar C Barriga G Folch C Gerpe A Cerecetto H González M 《Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy》2008,70(3):557-563
Cyclic voltammetry and electron spin resonance techniques were used in the investigation of novel 3-alkoxy- and 3-hydroxy-1-[omega-(dialkylamino)alkyl]-5-nitroindazole derivatives. A self-protonation process involving the protonation of the nitro group was observed. The reactivity of the nitro-anion radical for these derivatives with glutathione, a biological relevant thiol, was also studied by cyclic voltammetry. These studies demonstrated that glutathione could react with radical species from 5-nitroindazole system. Also we demonstrated that nitro-anion radicals show three different patterns of delocalization where the indazole 1-lateral chain does not have major influence. 相似文献