100423-08-3Relevant academic research and scientific papers
Design, synthesis, and in vitro evaluation of epigoitrin derivatives as neuraminidase inhibitors
Meng, Fanli,Yin, Yan,Lu, Cheng,Duan, Yongbin,Zhu, Yaohua,Huang, Chen,Zhou, Yiming,Xu, Xu,Wu, Fanhong
, p. 2037 - 2046 (2018)
Abstract: Influenza is an infectious disease which results in numerous epidemics every year. At present, neuraminidase is regarded, as the key therapeutic target against influenza and several well-known neuraminidase inhibitors are widely used as anti-influenza drugs. Combined computational methods including 3D-QSAR and molecular docking were applied to explore the structural–activity relationship with Xu’s compounds as the data set. Ten epigoitrin derivatives were then designed based on the computational results and they displayed 11.1–85.5?μM inhibitory potencies against neuraminidase in the in vitro biological evaluation. The combined computational studies did not only present the structural–activity relationship of Xu’s inhibitors, but also guide the designation of epigoitrin derivatives as novel neuraminidase inhibitors. Graphical abstract: [Figure not available: see fulltext.].
Direct catalytic synthesis of unprotected 2-amino-1-phenylethanols from alkenes by using iron(II) phthalocyanine
Legnani, Luca,Morandi, Bill
supporting information, p. 2248 - 2251 (2016/02/18)
Aryl-substituted amino alcohols are privileged scaffolds in medicinal chemistry and natural products. Herein, we report that an exceptionally simple and inexpensive FeII complex efficiently catalyzes the direct transformation of simple alkenes into unprotected amino alcohols in good yield and perfect regioselectivity. This new catalytic method was applied in the expedient synthesis of bioactive molecules and could be extended to aminoetherification.
Nucleophilic Aminomethylation of Aldehydes with α-Amino Alkylsilanes
Tsuge, Otohiko,Tanaka, Junji,Kanemasa, Shuji
, p. 1991 - 1999 (2007/10/02)
Fluoride-induced desilylation of (α-phthalimido-, α-morpholino-, and α-acetamidobenzyl)silanes and a (phthalimidomethyl)silane generates the corresponding α-amino carbanions which add to a variety of aldehydes.The conversion of phthalimido group of the adducts into amino moiety leads to β-amino alcohols.This simple reaction sequence offers a new and general method of nucleophilic aminomethylation.
