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马淑涛 教授


 

药物化学专业    马淑涛教授

 

一、基本情况

马淑涛山东临沂人。山东大学药学院药物化学教授,博士生导师。享受国务院特殊津贴,山东省科技进步一等奖获得者((第一位)),第七届山东省青年科技奖获得者。现任药物化学教研室主任。手机:15588877387

二、学习经历

198108月~198607月:山东医科大学药学系,获理学学士学位;

198808月~199107月:山东医科大学药学院,获理学硕士学位;

200408月~200706月:山东大学药学院,获理学博士学位

 三、工作经历

198608月~198807月:山东省临沂地区药品检验所,药师;

199108月~199210月:山东省医药工业研究所助理工程师

199211月~199612月:山东省医药工业研究所工程师

199701月~199710月:山东省医药工业研究所药物合成室副主任,工程师

199711月~200110月:山东省医药工业研究所药物合成室主任,副主任药师

200111月~200212月:山东省医药工业研究所药物合成室主任,主任药师

200301月~200409月:山东大学药学院,教授;

200410月~200707月:山东大学药学院,药物化学教研室主任,教授;

200708月~200808月:美国范德堡Vanderbilt大学化学系,访问学者

200809月~至今:山东大学药学院,药物化学教研室主任,教授。

 四、专业

    药物化学。

 五、研究方向与特色简介

1. 抗耐药菌先导化合物的发现、优化和相关化学生物学研究。

主要进行了以下研究工作: 基于靶点(例如,FtsZAcrB等)的抗耐药菌小分子化合物的设计、合成、抗菌活性和抗耐药机理研究。 复杂结构抗生素(例如,大环内酯类、糖肽类和脂肽类等)的结构修饰和构效关系研究。 重要抗菌天然产物(例如,海洋大环内酯类化合物)的全合成和作用机制研究。

2. 新药的开发研究

    主要开展了以下研究工作:⑴ 化学合成新药的制备工艺(包括实验室工艺和中试放大工艺)研究。⑵ 医药中间体和化工产品绿色制备工艺研究与开发。⑶ 杂质合成路线的设计与合成。

 六、主要科研成果

1. 阿奇霉素原料药新药证书,项目主持人,1997年;

2. 阿奇霉素胶囊剂药新药证书,项目主持人,1997年;

3. 低分子肝素钠(4000-6000)原料药新药证书,项目主持人,2001年;

4. 低分子肝素钠(4000-6000)注射液新药证书,项目主持人,2001年;

5. 地红霉素原料药新药证书,项目主持人,2003年;

6. 地红霉素肠溶片新药证书,项目主持人,2003年;

7. 地红霉素肠溶胶囊新药证书,项目主持人,2003年;

 七、近年发表的代表性论文

1. Li Jia, Shutao Ma*. Recent advances in the discovery of heparanase inhibitors as anticancer agents. Eur. J. Med. Chem. 2016, 121: 209–220.

2. Yinhu Wang, Henrietta Venter, Shutao Ma*. Efflux Pump inhibitors: A novel approach to combat efflux-mediated drug resistance in bacteria. Curr. Drug Targets 2016, 17: 702–719.

3. Di Song, Shutao Ma*. Recent development of benzimidazole-containing antibacterial agents. ChemMedChem 2016, 11, 646–659.

4. Shengsheng Qiang, Changde Wang, Henrietta Venter, Xin Li, Yi Wang, Liwei Guo, Ruixin Ma and Shutao Ma*. Synthesis and biological evaluation of novel FtsZ-targeted 3-arylalkoxy-2,6-difluorobenzamides as potential antimicrobial agents. Chem. Biol. Drug. Des. 2016, 87(2): 257–264.

5. Xin Li, Juzheng Sheng, Guihua Huang, Ruixin Ma, Fengxin Yin, Di Song, Can Zhao, Shutao Ma*. Design, synthesis and antibacterial activity of cinnamaldehyde derivatives as inhibitors of the bacterial cell division protein FtsZ. Eur. J. Med. Chem. 2015, 97: 32–47.

6. Yi Wang, Mi Yan, Ruixin Ma, Shutao Ma*. Synthesis and antibacterial activity of novel 4-bromo-1H-indazole derivatives as FtsZ inhibitors. Arch. Pharm. 2015, 348: 266–274.

7. Xin Li, Juzheng Sheng, Di Song, Liwei Guo, Shutao Ma*. Phenylacrylamides as novel FtsZ-targeted potential antimicrobials. Lett. Drug Des. Discov. 2015, 12(3): 234–240.

8. Mi Yan, Xiaodong Ma, Ruiqian Dong, Xin Li, Can Zhao, Zhenzhen Guo, Yan Shen, Fang Liu, Ruixin Ma, Shutao Ma*. Synthesis and antibacterial activity of 4"-O-(trans-β-arylacrylamido)carbamoyl azithromycin analogs. Eur. J. Med. Chem. 2015, 103: 506–515.

9. Xin Li, Shutao Ma*. Advances in the discovery of novel antimicrobials targeting the assembly of bacterial cell division protein FtsZ. Eur. J. Med. Chem. 2015, 95: 1–15.

10. Can Zhao, Yinhu Wang, Shutao Ma*. Recent advances on the synthesis of hepatitis C virus NS5B RNA-dependent RNA-polymerase inhibitors. Eur. J. Med. Chem. 2015, 102: 188–214.

11. Liwei Guo, Shutao Ma*. Advances in inhibitors of FXa. Curr. Drug Targets 2015, 16: 1207–1232.

12. Yan Shen, Shengsheng Qiang, Shutao Ma*. The Recent Development of Farnesyltransferase Inhibitors as Anticancer and Antimalarial Agents. Mini.Rev. Med. Chem. 2015, 15: 837–857.

13. Can Zhao, Shutao Ma*. Recent advances in the discovery of N-myristoyltransferase inhibitors. ChemMedChem 2014, 9: 2425 –2437.

14. Zhenzhen Guo, Shutao Ma*. Recent advances in the discovery of metallo-lactamase inhibitors for β-lactam antibiotic-resistant reversing agents. Curr. Drug Targets 2014, 15: 689–702.

15. Yuanze Wang, Shutao Ma*. Small molecules modulating AHL-based quorum sensing to attenuate bacteria virulence and biofilms as promising antimicrobial drugs. Shutao Ma*. Curr. Med. Chem. 2014, 21, 296–311.

16. Siti Ma, Chao Cong, Xiaohui Meng, Shasha Cao, Hongkun Yang, Yuanyuan Guo, Xueyi Lu, Shutao Ma*. Synthesis and on-target antibacterial activity of novel 3-elongated arylalkoxybenzamide derivatives as inhibitors of the bacterial cell division protein FtsZ. Bioorg. Med. Chem. Lett. 2013, 23: 4076–4079.

17. Xin Li, Shutao Ma*. Recent developments in the discovery of Novel antipsychotic agents modualating dopamine and serotonin receptors. Curr. Drug Targets 2013, 14, 899–918.

18. Xin Li, Siti Ma, Mi Yan, Yuanze Wang, Shutao Ma*. Synthesis and antibacterial evaluation of novel 11,4²-disubstituted azithromycin analogs with greatly improved activity against erythromycin-resistant bacteria. Eur. J. Med. Chem. 2013, 59: 209–217.

19. Siti Ma, Rongmei Wang, Yuanze Wang, Jichao Cao, Shutao Ma*. The synthesis and antibacterial activity of novel 3-O-arylalkylbenzamide derivatives as FtsZ inhibitors. Lett. Drug Des. Discov. 2013, 10, 320–326.

20. Yi Wang, Shutao Ma*.Recent advances in inhibitors of bacterial fatty acid synthesis type II (FASII) system enzymes as potential antibacterial agents. ChemMedChem 2013, 8, 1589–1608.

21. Mi Yan, Shutao Ma*. Recent advances in the research of heterocyclic Compounds as antitubercular agents. ChemMedChem 2012, 7: 2063–2075.

22. Siti Ma, Shutao Ma*. The development of FtsZ inhibitors as potential antibacterial agents. ChemMedChem. 2012, 7: 1161–1172.

23. Mi Yan, Jichao Cao, Xin Li, Siti Ma, Yuanze Wang, Chao Cong, Shutao Ma*. Synthesis and antibacterial activity of novel 11-O-phenethylcarbamoylazithromycin derivatives with 4²-elongated side chains. Lett. Drug Des. Discov. 2012, 9: 833–839.

24. Sean M. DeGuire, Shutao Ma, Gary A. Sulikowski. Synthesis of a bicyclobutane fatty acid identified from the cyanobacterium anabaena PCC 7120. Angew. Chem. Int. Ed., 2011, 50: 9940–9942.

25. Xiaodong Ma, Ling Zhang, Rongmei Wang, Jichao Cao, Chen Liu, Yi Fang, Jida Wang, Shutao Ma*. Novel C-4² modified azithromycin analogs with remarkably enhanced activity against erythromycin-resistant Streptococcus pneumoniae: The synthesis and antimicrobial evaluation. Eur. J. Med. Chem. 2011, 46: 5196–5205.

26. Chao Cong, Haiyang Wang, Yue Hu, Chen Liu, Siti Ma, Xin Li, Jichao Cao, Shutao Ma*. Synthesis and antibacterial activity of novel 4²-O-benzimidazolyl clarithromycin derivatives. Eur. J. Med. Chem. 2011, 46: 3105–3111.

27. Shutao Ma*, Bo Jiao, Yongjing Ju, Manjie Zheng, Ruixin Ma, Lin Liu, Ling Zhang, Xuecui Shen, Chenchen Ma, Ya Meng, Hui Wang, Yunkun Qi, Xiaodong Ma, Wenping Cui. Synthesis and antibacterial evaluation of novel clarithromycin derivatives with C-4² elongated arylalkyl groups against macrolide-resistant strains. Eur. J. Med. Chem. 2011, 46: 556–566.

28. Ling Zhang, Bo Jiao, Xiangrui Yang, Lin Liu, Shutao Ma*. Synthesis and antibacterial activity of new 4²-O-carbamates of 11,12-cyclic carbonate erythromycin A 6,9-imino ether. J. Antibiot. 2011, 64: 243–247.

29. Yunkun Qi, Ruixin Ma, Xin Li, Yue Hu, Siti Ma, Chao Cong, Xiaodong Ma, Wenping Cui, Shutao Ma*. Novel clarithromycin analogs with C-4² 2-arylbenzimidazolyl bishydrazide side chain: synthesis and antibacterial evaluation. Lett. Drug Des. Discov. 2011, 8: 966–971.

30. Xiaodong Ma, Shutao Ma*. Significant breakthroughs in search for anti-infectious agents derived from erythromycin A. Curr. Med. Chem. 2011, 18: 1993–2015.

31. Yunkun Qi, Shutao Ma*. The medicinal potential of promising marine macrolides with anticancer activity. ChemMedChem 2011, 6: 399–409.

32. Wenping Cui, Shutao Ma*. Recent advances in the field of 16-membered macrolide antibiotics. Mini-Rev. Med. Chem. 2011, 11:1009–1018.

33. Ling Zhang, Linchen Song, Zhaopeng Liu, Hui Li, Yingdong Lu, Zerong Li, Shutao Ma*. Synthesis and antibacterial activity of novel 3-O-carbamoyl derivatives of clarithromycin and 11,12-cyclic carbonate azithromycin. Eur. J. Med. Chem. 2010, 45: 915–922.

34. Yongjing Ju, Ruiqing Xian, Ling Zhang, Ruixin Ma, Jichao Cao, Shutao Ma*. Synthesis and antibacterial activity of novel 4²-O-arylalkylcarbamoyl and 4²-O-((arylalkylamino)-4-oxo- butyl)arbamoyl clarithromycin derivatives. Bioorg. Med. Chem. Lett. 2010, 20: 3272–3274.

35. Yunkun Qi, Bo Jiao, Xiaodong Ma, Wenping Cui, Shutao Ma*. Synthesis and antibacterial activity of novel 4²-O-carbamoyl erythromycin A derivatives. Arch. Pharm. 2010, 8: 458–464.

36. Ling Zhang, Shutao Ma*. Efflux pump inhibitors–a strategy to combat P-glycoprotein and NorA multidrug resistant pump. ChemMedChem 2010, 5: 811–22.

37. Chenchen Ma, Shutao Ma*. Various novel erythromycin derivatives obtained by different modifications: recent advance in macrolide antibiotics. Mini-Rev. Med. Chem. 2010, 10: 272–286.

38. Chenchen Ma, Zhaopeng Liu, Hualing Song, Rentao Jiang, Fawen He, Shutao Ma*. Synthesis and antibacterial activity of novel 11,12-cyclic carbonate azithromycin 4²-O-carbamate derivatives. J. Antibiot. 2010, 63: 3–8.

39. Xuecui Shen, Bo Jiao, Shutao Ma*. Synthesis and antibacterial activity of 4²-O-carbamoyl analogs of clarithromycin. Chin. Chem. Lett. 2010, 21: 257–260.

40. Shutao Ma*, Ruixin Ma, Zhaopeng Liu, Chenchen Ma, Xuecui Shen. Synthesis and antibacterial activity of novel 15-membered macrolide derivatives: 4²-carbamate, 11,12-cyclic carbonate-4²-carbamate and 11,4²-di-O-arylcarbamoyl analogs of azithromycin. Eur. J. Med. Chem. 2009, 44: 4010–4020.

41. Shutao Ma*, Bo Jiao, Zhaopeng Liu, Hui Wang, Ruiqing Xian, Manjie Zheng, Hongxiang Lou. Synthesis and antibacterial activity of 4²,11-di-O-arylalkylcarbamoyl azithromycin derivatives that have activity against resistant strains, Bioorg. Med. Chem. Lett. 2009, 19: 1698–1701.

42. Shutao Ma*, Ruixin Ma, Ruiqing Xian, Bo Jiao. Synthesis of novel 15-membered macrolide dimers. Chin. Chem. Lett. 2009, 20: 931–934.

* 通讯作者.

 八、获得专利

1. 阿奇霉素4²-氨基甲酸酯衍生物、制备方法及其药物组合物,专利号:ZL200710015049.4

2. 11,12-环碳酸酯-阿奇霉素4²-氨甲酸酯衍生物、制备方法及其药物组合物,专利号:ZL200710015050.7

3. 11,4²-二氨基甲酸酯阿奇霉素衍生物、制备方法及其药物组合物,专利号:ZL200810238167.6

4. 阿奇霉素衍生物、制备方法及中间体,专利号:ZL201010224599.9

5. 4²-芳烷基氨基甲酸酯克拉霉素衍生物、制备方法及其药物组合物,专利号:ZL201010011838.2

6. 4²-苯并咪唑-5-甲酰基-肼基甲酸酯克拉霉素衍生物及中间体,专利号:ZL201010224597.X

7. 4²-((取代苯甲酰胺基)烷基)氨基甲酸酯阿奇霉素11-氨基甲酸酯衍生物及其中间体,专利号:ZL201110146229.2

8. 末端含吸电子基取代的4²-O-氨基甲酸酯类克拉霉素衍生物及其中间体制备方法和应用,专利号:ZL201200002065.0

9. 4²-O-(反式-β-芳基烯丙酰胺)氨基甲酰基阿奇霉素衍生物,专利号:ZL201210240489.0

10. 4"-O-(1-芳烷基-1,2,3-三氮唑-4-甲基-氨基甲酰基)阿奇霉素衍生物,2015.10.21,专利号:ZL201310241948.1

 九、出版著作

副主编出版著作:《药物化学(案例版)》第一版,科学出版社,北京,2010年;

参编的著作:《药物化学(案例版)》第二版,科学出版社,北京,2016年;《药物化学(案例版)笔记与考试复习指南》,科学出版社,北京,2016年。

 十、荣誉奖励

1. 阿奇霉素及胶囊剂的研究,荣获山东省科技进步一等奖(第一名),证书编号:第00-1-9-1号,2000

2. 国务院政府特殊津贴,证书编号:第03702010号,2002

3. 第七届山东省青年科技奖,2002

 

联系方式:E-mailmashutao@sdu.edu.cn;地址:济南市文化西路44  山东大学药学院,邮编250012


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