Sulfur, selenium and tellurium containing amines act as effective carbonic anhydrase activators
作者:Damiano Tanini、Antonella Capperucci、Claudiu T. Supuran、Andrea Angeli
DOI:10.1016/j.bioorg.2019.03.062
日期:2019.6
A new series of β-aminochalcogenides were designed and synthesized to identify new carbonic anhydrase activator (CAA) agents as novel tools for the management of several neurodegenerative and metabolic disorders which represent a clinical challenge without effective therapies available. Some β-aminoselenides and β-aminotellurides showed effective CA activating effects and a potent antioxidant activity
The efficient and mild copper-catalyzed synthesis of unsymmetrical diorganyl chalcogenides under ligand- and solvent-free conditions is described. The cross-coupling reaction was performed using aryl boric acids and 0.5 equiv. of diorganyl dichalcogenides (Te/Se/S) in the presence of 3 mol % of CuI and 3 equiv. of DMSO, under microwave irradiation. This new protocol allowed the preparation of several
A greener protocol for the synthesis of phosphorochalcogenoates: Antioxidant and free radical scavenging activities
作者:Daniela H. Mailahn、Lucas E.B. Iarocz、Patrick C. Nobre、Gelson Perin、Airton Sinott、Ana Paula Pesarico、Paloma T. Birmann、Lucielli Savegnago、Márcio S. Silva
DOI:10.1016/j.ejmech.2020.113052
日期:2021.3
which this stability study was also important to select some products for pharmacological screening. The phosphorochalcogenoates were screened in vitro and ex vivo tests for the antioxidant potential and free radical scavenging activity, as well as to investigation toxicity in mice through of the plasma levels of markers of renal and hepatic damage. The pharmacological screening of phosphorochalcogenoates
在这一贡献中,已开发出一种无金属和碱的方案,用于通过在50°C下使用DMSO作为溶剂来合成磷碳氢酸盐(Se和Te)。由二有机基二卤代膦酸酯和H-膦酸酯制备了多种磷代碳氢酸酯,导致了Chal-P(O)键的形成,反应速度快,收率好至极佳。通过1D和2D NMR,IR,CGMS和HRMS分析获得了产品的完整结构说明,并进行了磷藻酸酯的稳定性评估以有效地描述这种简单可行的方法。典型77硒 1个H}(δ硒= 866.0 ppm)设为125碲 1个H}(δTE = 422.0 PPM)和31 p 1个H}(δ P = -1.0,-13.0 -15.0和PPM)NMR化学位移均必须确认的副产物,其中该稳定性研究也很重要选择一些产品的药理学筛选。在体外和离体中筛选了磷酸胆碱酯进行抗氧化剂潜力和自由基清除活性测试,并通过血浆肾脏和肝损伤标志物的水平调查小鼠的毒性。药代磷酸酯的药理学筛选表明,该化合物
Mercapto acid compounds of tellurium(II): stabilization of telluriumsulfur bonded compounds via intramolecular chelation
作者:Sylvia A. Gardner
DOI:10.1016/s0022-328x(00)90629-6
日期:1980.5
Bis(benzenethio)tellurium(II) and bis(2-naphthalenethio)tellurium(II) have been synthesized and are unstable both in the solid state and in solution. Nixed derivatives containing one aryl and one sulfide bonded to tellurium (ArTeSCH2CH2COOH) have also been prepared, and the reactions of these compounds with dichlorobis(benzonitrile)palladium(II) yield palladium complexes containing two tellurium ligands.
Discovery of new 2, 5-disubstituted 1,3-selenazoles as selective human carbonic anhydrase IX inhibitors with potent anti-tumor activity
作者:Andrea Angeli、Elena Trallori、Marta Ferraroni、Lorenzo Di Cesare Mannelli、Carla Ghelardini、Claudiu T. Supuran
DOI:10.1016/j.ejmech.2018.08.096
日期:2018.9
range, and were evaluated for their effects on cell viability against the human prostate (PC3) and breast (MDA-MB-231) cancer cell lines, showing effective anti-tumoractivity. These selenazoles are interesting leads for the development of new, isoform-selective CA IX inhibitors.