Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Eur J Med Chem. 2021 Jan 1;209:112885. doi: 10.1016/j.ejmech.2020.112885. Epub 2020 Sep 28.
In recent years, interest in sulfoximine chemistry has been greatly increased. For example, at least three sulfoximine containing drugs BAY 1143572, BAY 1251152 and AZD6738 have entered the clinic. Despite the increasing interest in sulfoximines and their chemistry, the routine application of this structure in drug discovery is still hampered due to limited experience in physicochemical and in vitro parameters of sulfoximines. Therefore, we reviewed all relevant articles from 2013 to the present in terms of potency and pharmacokinetic properties in order to support the addition of the sulfoximine component to the toolbox of medicinal chemists.
近年来，人们对亚砜亚胺化学的兴趣大大增加。例如，至少有三种含亚砜亚胺的药物 BAY 1143572、BAY 1251152 和 AZD6738 已进入临床阶段。尽管人们对亚砜亚胺及其化学性质越来越感兴趣，但由于在亚砜亚胺的理化和体外参数方面经验有限，因此该结构在药物发现中的常规应用仍受到阻碍。因此，我们回顾了 2013 年至今所有相关的文章，内容涉及在效力和药代动力学性质方面的研究，以支持在药物化学家的工具包中添加亚砜亚胺成分。
