科学研究情况简介
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【近5年来主要研究课题】 1. 从事基于天然产物的创新药物研究:从天然产物中发掘苗头化合物,对苗头分子进行全合成及靶向性的结构优化,近年来已发现一些具有成药性的先导化合物,用以治疗糖尿病、慢性阻塞性肺炎、肺动脉高压等重大慢性疾病。 2. 从事有机合成新方法的研究:开发高效的有机合成新方法来构建多样性的类药性分子实体(杂环化合物),而后进行活性筛选,助力药物先导分子的发现。 【近5年来主持项目】 1. 国家自然科学基金面上项目:新骨架PKC系列抗炎天然分子的发现与研究(22177121);2022.01-2025.12 2. 上海市自然科学基金面上项目:天然抗炎活性物质的发现、合成及活性研究(20ZR1467800);2020.07-2023.06 3. 国家自然科学基金青年基金:抗COPD高选择性PDE4天然抑制剂的发现:SelaginpulvilinK的结构优化和生物活性研究(81703341);2018.01-2020.12 【近5年来代表性论文】 1) Kai-Wen Hu#, Xiao You#, Jin-Zheng Wang, Xiaoan Wen, Hongbin Sun,* Qing-Long Xu,*, Zengwei Lai*.Chiral Phosphoric Acid Catalyzed Asymmetric Desymmetrization of para-Quinamines with Isocyanates: Access to Functionalized Imidazolidin-2-one Derivatives. Org. Lett. 2021, 23(20), 7873-7877. 2) Zengwei Lai#, Renwei Zhang#, Qiang Feng, Jianwei Sun*. 3-Aminooxetanes: Versatile 1,3-Amphoteric Molecules for Intermolecular Annulation Reactions. Chem. Sci. 2020, 11, 9945-9949. (#:equal contribution) 3) Tianhua Zhang#, Zengwei Lai#, Shuyin Yuan, Yi-You Huang, Guoqiang Dong, Chunquan Sheng*, Hengming Ke*, Hai-Bin Luo*. Discovery of Evodiamine Derivatives as Highly Selective PDE5 Inhibitors Targeting a Unique Allosteric Pocket. J. Med. Chem. 2020, 63, 17, 9828-9837. (#:equal contribution) 4) Chen Zhang, Qian Zhou, Xu-Nian Wu, Ya-Dan Huang, Jie Zhou, Zengwei Lai*, Yinnuo Wu*, Hai-Bin Luo. Discovery of novel PDE9A inhibitors with antioxidant activities for treatment of Alzheimer’s disease. J. Enzym. Inhib. Med. Chem. 2018, 33(1), 260-270. 5) Zeng-Wei Lai, Chuan Liu, Hongbin Sun*, Shu-Li You*. Asymmetric Synthesis of 3-Allyloxindoles and 3-Allenyloxindoles by Scandium(III)-catalyzed Claisen Rearrangement Reactions. Chin. J. Chem. 2017, 35(10), 1512-1516. 【以往重要代表性论文】 1) Zengwei Lai, Zhaobin Wang, Jianwei Sun*. Organocatalytic Asymmetric Nucleophilic Addition to ortho-Quinone Methides by Alcohols. Org. Lett. 2015, 17(24), 6058-6061. 2) Zeng-Wei Lai, Chunhong Li, Jun Liu, Lingyi Kong, Xiaoan Wen*, Hongbin Sun*. Discovery of Highly Potent DPP-4 Inhibitors by Hybrid Compound Design Based on Linagliptin and Alogliptin. Eur. J. Med. Chem. 2014, 83, 547-560. 3) Yu-Rong Yang*, Zeng-Wei Lai, Liang Shen, Jiu-Zhong Huang, Xing-De Wu, Jun-Lin Yin and Kun Wei. Total Synthesis of (-)-8-Deoxyserratinine via an Efficient Helquist Annulation and Double N-Alkylation Reaction. Org. Lett. 2010, 12(15), 3430-3433. 【近5年主要授权专利】 1) 一种1,1’-二茂铁全氟烷基膦氮配体、其制备方法及应用. CN 201410065244.8. 2) 一类吴茱萸碱类化合物及其制备方法与应用. CN 201710245872.8.
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