简单介绍

吴一诺 博士,副教授,硕士研究生导师。2006年本科毕业于中山大学化学与化学工程学院应用化学专业。2011年毕业于中山大学药学院药物化学专业,获理学博士学位。2011年至2013年于香港理工大学应用生物与化学科技系进行博士后研究。2013年加入中山大学药学院。主要从事磷酸二酯酶抑制剂的发现 及其在神经系统疾病中的应用。目前已在Org. Lett., Chem.Commun., J. Med.Chem, E.  J. Med.Chem, Chem.Eur. J., Adv. Synth. Catal.等国际权威杂志发表SCI收录论文30余篇。共主持国家自然科学基金等项目7项,并作为课题骨干参与国家科技部重点研发计划。

教育经历

2006/09 - 2011/06,中山大学,药学院,药物化学,博士

2002/09 - 2006/06,中山大学,化学与化学工程学院,应用化学系,学士

 

工作经历

 

 

2018/04- 至今,中山大学,药学院,副教授

2013/07 - 2018/04,中山大学,药学院,讲师

2011/07 - 2013/06,香港理工大学,应用生物与化学科技系,博士后

 

 

教学情况

《现代分析技术与应用》

《基础化学实验》

科研项目

1. 国家自然科学基金青年项目,钯催化下甲苯类酰化试剂参与的邻位和间位C-H酰基化反应,项目编号:21402243;2015.01 - 2017.12; 25万元

2. 国家重点研发计划,课题骨干,基于E 级高性能计算生物医药应用软件系统研制及应用。课题四:癌症、糖尿病与感染性疾病新药研究与软件应用验证, 课题编号:2017YFB0202604; 2017.07 - 2020.12; 749万元。

3. 广州市科技计划项目珠江科技新星专题,新型萘内酰亚胺类磷酸二酯酶二型抑制剂的合理化设计、合成及其抗阿尔茨海默症药效研究,2018.01 - 2020.12;30万元。

4. 广东省医学科研基金,C-H键磷酯方法高效构建HIV-1非核苷类逆转录酶抑制剂,项目编号:B2014106;2014.06 - 2016.06;1万元。

5. 广东省中医药局面上项目,透骨草中天然磷酸二酯酶4型抑制剂的发现及结构改造,项目编号:20171049;2017.01 - 2018.12;0.5万元。

6. 中山大学青年教师培育基金,C-H键磷酯方法高效构建苯(杂)环类有机磷化合物新型方法研究,项目编号:13ykpy10;2013.11 - 2016.12;15万元。

7. 中山大学青年教师起步基金,钯催化C-H酰基化反应在芳(杂)环酮类物质制备中的应用,项目编号:31101402;2013.11 - 2014.12;2万元。

8. 国家自然科学基金青年项目,合作单位负责人,可支配经费10万元;吡喃并吡唑类AKR1C3选择性抑制剂的设计、优化和分子机制研究,项目编号:81602968;2017.01 - 2019.12

 

论著专利

        近年来共发表论文35篇,其中第一作者或共同通讯作者论文23篇,8篇属于中科院JCR分区一区论文;总引用次数884次,单篇最高他引次数为125次。以第二发明人申请中国专利2项,第三发明人申请欧洲专利1项。

部分第一或通讯作者发表论文列表如下:

 

1.     Yu, Y. F.; Huang, Y. D.; Zhang, C; Wu, X. N.; Zhou, Q; Wu, D. Y.; Wu, Yinuo*;  Luo, H. B. Discovery of Novel Pyrazolopyrimidinone Derivatives as  Phosphodiesterase 9A Inhibitors Capable of Inhibiting  Butyrylcholinesterase for Treatment of Alzheimer's Disease. ACS Chem. Neurosci2017, 8, 2522. 

 

2.  Zhang, C.; Zhou, Q.; Wu, X. N.; Huang, Y. D.; Zhou, J.; Lai, Z.; Wu, Yinuo*; Luo, H.-B. Discovery of novel PDE9A inhibitors with antioxidant activities for treatment of Alzheimer’s disease. J. Enzym. Inhib. Med. Chem. 2017, Just Accepted. DOI: 10.1080/14756366.2017.1412315.

3.  Zhang, C; Feng, L. J.; Huang, Y. Y.; Wu, D. Y.; Li, Z.; Zhou, Q.; Wu, Yinuo*;  Luo,  H. B.* Discovery of Novel Phosphodiesterase-2A Inhibitors by  Structure-Based Virtual Screening, Structural Optimization, and  Bioassay. J. Chem. Inf. Model. 2017, 57, 355.

 

4.  Wu, X. N.; Huang, Y. D.; Li, J.; Yu, Y.-F.;Zhou, Q.; Zhang, C.; Wu, Yinuo* and Luo, H.-B.* Structure-based design, synthesis, and biological evaluation of novel pyrimidinone derivatives as PDE9 inhibitors. Acta Pharmaceutica Sinica B. 2017, Just Accepted. 

5. Zheng, X. H.; Zhou, S. Y.; Zhang, C.; Wu, D. Y.; Luo, H. B.; Wu, Yinuo* Docking-assisted 3D-QSAR studies on xanthones as alpha-glucosidase inhibitors. J. Mol. Model. 201723, DOI: 10.1007/s00894-017-3438-1. 

 

6.   Tan, B.X.; Yang, L.; Huang, Y. Y.; Chen, Y. Y.; Peng, G. T.; Yu, S.; Wu, Yinuo*; Luo, H. B.; He, X. X. Bioactive triterpenoids from the leaves of Eriobotrya japonica as the natural PDE4 inhibitors. Natural Product Research, 2017, 31, 2836.

7. Zheng, X.; Wu, X. N.; Chen, J. Y.; Luo, H. B.; Wu, D.*; Wu, Yinuo*. Transitional Metal-free catalyzed C-H arylation of unactivated arenes with 8-hydroxyquinoline as a promoter.Synthesis 2017,Just Accepted.

 

8.    Wu, Yinuo Jiang, C.; Wu, D.; Gu, Q.; Luo, Z. Y.; Luo, H. B.*. Palladium-catalyzed  C–H bond carboxylation of acetanilides: an efficient usage of N,  N-dimethyloxamic acid as the carboxylate source. Chem. Commun. 2016, 52, 1286.

9.  Wu, YinuoSun, L.; Chen, Y.; Zhou, Q.; Huang, J. W.; Miao, H.; Luo, H. B.* Palladium-catalyzed decarboxylative acylation of N-nitrosoanilines with α-oxocarboxylic acids. J. Org. Chem. 2016, 81, 1244.

 

10.      Cai, Y. H.; Guo, Y.; Li, Z.;Wu, D.; Li, X.; Zhang, H.; Yang, J.; Lu, H.; Sun. Z.; Luo, H. B.; Yin, S.*;  Wu, Yinuo*. Discovery and modelling studies of natural ingredients from Gaultheria yunnanensis (FRANCH.) against phosphodiesterase-4. Eur. J. Med. Chem. 2016114, 134.

 

11.   Yang, Q. J.; Choy, P. Y.; Wu, Yinuo*; Fan, B. M.*; Kwong, F. Y.* Oxidative coupling between C(sp(2))-H and C(sp(3))-H bonds of indoles and cyclic ethers/cycloalkanes. Org. Biomo. Chem. 2016, 14, 2608. 

 

12.   Li, Z.; Lu, X.; Feng, L.-J.; Gu, Y.; Li, X.; Wu, Yinuo*; Luo, H.-B.* Molecular dynamics-based discovery of novel phosphodiesterase-9A inhibitors with non-pyrazolopyrimidinone scaffolds. Mol. BioSyst. 2015, 11, 115.

13.      Wu, Yinuo; Feng, L. J.; Lu, X.; Kwong, F. Y.*; Luo, H. -B.*. Palladium-catalyzed oxidative C–H bond acylation of N-nitrosoanilines with toluene derivatives: a traceless approach to synthesize N-alkyl-2-aminobenzophenones. Chem. Commun. 2014, 50, 15352.

 

14.   Wu, Yinuo*; Choy, P. Y.; Kwong, F. Y. Direct intermolecular C–H arylation of unactivated arenes with aryl bromides catalysed by 2-pyridyl carbinol. Org. Biomo. Chem. 2014, 12, 6820.

15.   Wu, Yinuo; Choy, P. Y.; Kwong, F. Y.* A Direct C-H Arylation of Unactivated Arenes Promoted by Mixed Potassium Alkoxides. Asian J. Org. Chem. 2014, 3, 1262.

16.    Wu, Yinuo; Choy P. Y., Mao F., Kwong F. Y.* Toluene Derivatives as Simple Coupling Precursors for Cascade Palladium-Catalyzed Oxidative C-H bond Acylation of Acetanilides. Chem. Commun. 201349, 689.

 

17.   Wu, Yinuo; Kwong, F. Y.; Li, P. ; Chan, A. S. C.  An Efficient Oxidative Cross-Coupling Reaction between CH and NH Bonds; A Transition-Metal-Free Protocol at Room Temperature. Synlett, 2013, 24, 2009.

18.       Wu, Yinuo; Wong, S. M.; Mao, F.; Chan, T. L.; Kwong, F. Y. * Intramolecular Direct C-H Bond Arylation from Aryl Chlorides: A Transition-Metal-Free Approach for Facile Access of Phenanthridines. Org. Lett. 2012, 14, 5306.

19.   Wu, Yinuo; Wang, J.; Li, P. *; Kwong, F. Y.* Catalyst-free efficient aza-michael addition of azoles to nitroalkenes, Synlett201223, 788.

20.    Wu, Yinuo; Li, B.; Mao, F.; Li, X.;* Kwong, F. Y.* Palladium -Catalyzed Oxidative C-H Bond Coupling of Steered Acetanilides and Aldehydes: A Facile Access to ortho-Acylacetanilide. Org. Lett. 201113, 3258.

21.      Wu, Yinuo; Mao, F.; Meng, F.; Li. X.* Enantioselective Vanadium-Catalyzed Oxidation of 1,3-Dithianes from Aldehydes and Ketones using beta-Amino Alcohol Derived Schiff Base Ligands. Adv. Synth.Catal. 2011, 353, 1707.

 

22.   Wu, Yinuo; Wang, J. *; Mao, F.; Kwong F. Y.*Palladium-catalyzed cross-dehydrogenative functionalization of C (sp (2))-H Bonds. 综述Chem. Asian J. 2014, 9, 26.

23.   Chan T. L.; Wu, Yinuo*Choy P. Y.; Kwong F. Y.* A Radical Process towards the Development of Transition Metal-Free Aromatic Carbon-Carbon Bond-Forming Reactions. 综述Chem. Eur. J. 201319, 15802

 

专利:

1.    Wu, YinuoWang, J.;Kwong F. Y. C-C Cross-Coupling Reactions of Acidic C-H Nucleophiles with Two Activating Groups, Science of synthesis, Cross Coupling and Heck-Type Reactions 2. 2.7.2. 2012年11月21日

2.       Luo, Haibin; Wu, Yinuo; Deng, Yalin; Huang, Yiyou; Wu, Xunian .Preparation of quinazoline compounds as inhibitors of phosphodiesterase type 10。专利号:CN 106632089;专利申请日:2016年9月4日,专利类型:A,公开日期:2017年5月10日

3.      Luo, H. B.; Wu, Yinuo; Wu, X.; Huang, Y.; Zhou, Q.  N-Substituted pyrazolo[3,4-d]pyrimidinone compound, preparation method and application thereof。专利号:CN 106977518;专利申请日:2017年3月6日,专利类型:A,公开日期:2017年7月25日

4.      Kwong, Fuk Yee; Choy, Pui Ying; Wu, Yinuo; Yang, Qingjing Synthesis of phosphine ligands bearing tunable linkage and methods of their use in catalysis,专利号:WO2017193288;专利申请日:2016年5月10日,专利类型:A1,公开日期:2017年9月16日