41067-80-5Relevant articles and documents
Reactions of Aminoacetals with C-Nucleophiles as a New Method for the Synthesis of Di(het)arylmethane Derivatives with a Taurine Fragment
Bekrenev, D. D.,Burilov, A. R.,Gazizov, A. S.,Pudovik, M. A.,Smolobochkin, A. V.,Yakhshilikova, L. J.
, p. 161 - 165 (2022/03/18)
Abstract: Based on the acid-catalyzed reaction of functionalized aminoacetals with C-nucleophiles, a series of new diarylmethane derivatives with a taurine fragment were synthesized, the structure of which was established by NMR spectroscopy method.
Development of Selective Steroid Inhibitors for the Glucose-6-phosphate Dehydrogenase from Trypanosoma cruzi
Fredo Naciuk, Fabrício,Do Nascimento Faria, Jéssica,Gonc?lves Eufrásio, Amanda,Torres Cordeiro, Artur,Bruder, Marjorie
supporting information, p. 1250 - 1256 (2020/07/27)
Chagas disease is a parasitic infection affecting millions of people across Latin America, imposing a dramatic socioeconomic burden. Despite the availability of drugs, nifurtimox and benznidazole, lack of efficacy and incidence of side-effects prompt the identification of novel, efficient, and affordable drug candidates. To address this issue, one strategy could be probing the susceptibility of Trypanosoma parasites toward NADP-dependent enzyme inhibitors. Recently, steroids of the androstane group have been described as highly potent but nonselective inhibitors of parasitic glucose-6-phosphate dehydrogenase (G6PDH). In order to promote selectivity, we have synthesized and evaluated 26 steroid derivatives of epiandrosterone in enzymatic assays, whereby 17 compounds were shown to display moderate to high selectivity for T. cruzi over the human G6PDH. In addition, three compounds were effective in killing intracellular T. cruzi forms infecting rat cardiomyocytes. Altogether, this study provides new SAR data around G6PDH and further supports this target for treating Chagas disease.
Chemo- and Regioselective Direct Functional Group Installation through Catalytic Hydroxy Group Selective Conjugate Addition of Amino Alcohols to α,β-Unsaturated Sulfonyl Compounds
Li, Zhao,Yazaki, Ryo,Ohshima, Takashi
supporting information, p. 3350 - 3353 (2016/07/26)
A chemoselective functional group installation through catalytic hydroxy group selective conjugate addition of amino alcohols to a variety of functionalized α,β-unsaturated sulfonyl derivatives was developed. Azide group installation for click chemistry and facile fluorescent labeling onto the less reactive hydroxy group demonstrated the synthetic utility of the present chemoselective catalysis. Moreover, chemo- and regioselective reaction of an unprotected amino diol was achieved for the first time.
