【近年来获得的学术科研成果】 主持和参加了国家自然科学基金计划、国家重大新药创制专项、中国科太阳娱乐新药研究科技专项、部省级科研计划和企业合作项目近10项,主持完成项目5项。获行业科技进步奖1次,公开和获得授权国家发明专利共计20项。在包括Journal of Medicinal Chemistry、European Journal of Medicinal Chemistry、Journal of Biological Chemistry、 Journal of Organic Chemistry、ChemMedChem和Bioorganic & Medicinal Chemistry Letters等国内外重要学术期刊发表论著30余篇。 【近年来主要研究课题】 [1] 共价结合药物研发技术,重大新药创制科技重大专项(2018ZX09711002-007-001),主持在研 [2] E76K突变型蛋白酪氨酸磷酸酶SHP2变构抑制剂的设计、连续化合成及抗髓系白血病活性研究,国家自然科学基金面上项目( 21772068 ),主持在研 [3] E76K突变型蛋白酪氨酸磷酸酶SHP2变构抑制剂的设计、合成及构效关系研究,新药研究国家重点实验室开放课题(SIMM1705KF-01)主持在研 [4] 基于连续流化学技术的新型吖啶酯化学发光诊断试剂的研发,江苏省政策引导类计划(产学研合作)前瞻性联合研究项目(BY2016022-37)主持在研 [5] 新型SHP2选择性抑制剂设计、合成及构效关系研究,主持国家自然科学基金面上项目(21472069)主持结题 [6] 新型抗血吸虫药物的发现及结构优化,卫生部寄生虫病预防与控制技术重点项目(WK014-002)主持结题 【近年来主要代表作】 [1] Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitor. Bioorganic & Medicinal Chemistry Letters. 2018, 24, 1889–1894. [2] Decoquinate derivatives: A new class of potent antischistosomal agents against Schistosoma japonicum. Chinese Chemical Letters. 2017, 28(7), 1547-1552. [3] Synthesis of Aromatic Amide Derivatives and Their Biological Evaluation against Protein Tyrosine Phosphatase 1B and Scr Homology-2 Domain Containing Protein Tyrosine Phosphatase-2. Chinese. Journal of Organic Chemistry. 2016, 36(9), 2142-2149. [5] Synthesis of Novel 3-aryl-1-oxa-2,8-diazaspiro[4.5]dec-2-ene Derivatives and Their Biological Evaluation Against Protein Tyrosine Phosphatase 1B. Chemical Biology & Drug Design 2015, 86(5), 1161–1167. [6] Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors. Bioorganic & Medicinal Chemistry Letters 2014, 24, 1889-1894. [7] 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors. Molecules. 2014, 19, 102-121. [8] Synthesis and evaluation of the antischistosomal activity against S. japonicum of 1-methyl-1,2,3,4-tetrahydroisoquinoline derivatives. Chinese. Journal of Organic Chemistry. 2013, 33, 2588-2599. [9] Synthesis and SAR studies of praziquantel derivatives with activity against Schistosoma japonicum. Molecules. 2013, 18(8), 9163-9178. [10] Synthesis and antiviral activity of conformational analogues of leucamide A. Molecules. 2012, 17(12), 14522-14530. [11] Synthesis and biological evaluation of salicylate-based compounds as a novel class of methionine aminopeptidase inhibitors. Bioorganic & Medicinal Chemistry Letters. 2011, 21(23), 7151-7154. [12] Inhibition of Mycobacterium tuberculosis Methionine Aminopeptidases by Bengamide Derivatives. ChemMedChem. 2011, 6, 1041-1048. [13] Growth inhibition of Escherichia coli and methicillin-resistant Staphylococcus aureus by targeting cellular methionine aminopeptidase. European Journal Medicinal Chemistry 2011, 46, 3537-3540. [14] Searching for Disease Modifiers - PKC Activation and HDAC Inhibition - A Dual Drug Approach to Alzheimer’s Disease that Reduces Aβ Production while Blocking Oxidative Stress. ChemMedChem. 2009, 4, 1095-1105. [15] Synthesis and structure-function analysis of Fe(II)-form-selective antibacterial inhibitors of Escherichia coli methionine aminopeptidase, Bioorganic & Medicinal Chemistry Letters. 2009, 19, 1080-1083. [16] Fe(II) is the native cofactor for Escherichia coli methionine aminopeptidase. Journal of Biological Chemistry. 2008, 283, 26879-26885. [17] Discovery of inhibitors of Escherichia coli methionine aminopeptidase with the Fe(II)-form selectivity and antibacterial activity. Journal of Medicinal Chemistry. 2008, 51, 6110-6120. [18] Discovery and Structural Modification of Inhibitors Of Human Hepatitis B Virus inspired from marine natural product Leucamide A. ChemMedChem. 2008, 3, 1316-1321. [19] Synthesis and biological evaluation of novel bisheterocycle-containing compounds as potential anti-influenza virus agents. Bioorganic & Medicinal Chemistry Letters. 2005, 15(23), 5284-5287. [20] First total synthesis of leucamide A. Journal of Organic Chemistry. 2003, 68(4), 1636-1639. 【主要授权国家发明专利】 [1] 一类2,3-二氢萘嵌间二氮杂苯类似物、其合成方法、药物组合物及用途(ZL201310365517.6) [2] 一类苯环-芳香环串联化合物、其制备方法和医药用途(ZL201410030074.X) [3] 一类螺异噁唑啉衍生物、其制备方法及医药用途(ZL201410112206.3) [4] 一类1,2,5-噁二唑-2氧化物类似物、其制备方法和用途(ZL201310298298.4) [5] 一类吡喹酮类似物、其制备方法和用途(ZL201310007886.8) |