傅晓钟
2016-12-27 10:56

傅晓钟,博士,教授,硕士研究生导师(学术硕士导师),贵州医科大学药物化学教研室主任,药物化学学科组负责人,药学院党委委员,贵州省第九批优秀青年科技人才培养对象,贵州省优秀教师,中组部第十批“西部之光”访问学者,国家职业资格鉴定高级考评员,国家自然科学基金通讯函评专家,科学出版社药学本科《药物化学》“十三五”规划教材副主编。国际著名学术期刊Journal of Medicinal Chemistry, Medicinal Chemistry Research, Journal of Pharmacy and Pharmacology , Current Medicinal Chemistry杂志审稿人。

一、主要研究方向

1、基于主动转运机理的黄酮类天然活性成分的结构修饰、生物活性及其构效关系研究;

2、基于脑靶向性转运性质的黄酮类天然活性成分设计、合成、生物活性及其构效关系研究;

3、基于肝靶向性增强与毒性降低的核苷类抗病毒药物研究;

4、具有主客体包合作用特性与特定释放规律的药物-瓜环(Cucurbit[n]uril)分子药物胶囊的设计与合成;

二、主持的代表性研究项目

1、基于脑靶向性转运机制的灯盏乙素苷元衍生物设计与合成, 国家自然科学基金(No. 81260473)

2、基于肝靶向性转运机制的阿德福韦单L-氨基酸酯,单胆酸酯衍生物的设计、合成与生物活性研究,国家自然科学基金(No. 81460523)

3、基于肾毒性降低与抗乙肝病毒活性增强的阿德福韦前药设计与合成, 国家自然科学基金(No. 20962004)

4、灯盏乙素及其苷元L-氨基酸氨基甲酸酯类衍生物的设计、合成及抗氧化作用机制研究,贵州省优秀青年科技人才培养对象专项资金(黔科合人字2013-45号)

5、基于肝靶向性转运机制的阿德福韦胆酸衍生物的设计与合成, 贵州省社会发展攻关计划项目(No. 2013-3031号)

6、基于脑靶向性转运机制的灯盏乙素苷元衍生物设计与合成, 贵州省中药现代化科技产业研究开发专项(黔科合ZY字2012-3013号)

7、药物化学“一流课程”建设,贵州省教育厅(2017年立项)

三、发表代表性研究论文、会议论文、专利和获得学术奖励情况

(一)期刊论文

1. Yongxi Dong, Li Dong,Jinglei Chen, Min Luo, Xiaozhong Fu*, Chunhua Qiao Synthesis and biological evaluation of N-alkyl-1,4-dihydroquinoline prodrugs of scutellarin methyl ester as neuroprotective agents. Med Chem Res. 2018, 27, 1111-1121.

2. Zhao, Y.-L.*; Tang, Y.-Q., Fei, X.-H.; Xiao, T.; Lu, Y.-D.; Fu, X.-Z.; He, B.; Zhou, M; Li, C; Xu, P.-F.* Yang, Y.-Y.*. Palladium-Catalyzed Direct C(sp3)-H Arylation of Indole-3-ones with Aryl Halides: A Novel and Efficient Method for the Synthesis of Nucleophilic 2-Monoarylated Indole-3-ones. RSC Adv. 2018, 8, 25292- 25297.

3. Ya Chen, Wen Zheng Zhang, Jing Li, Tao Xiao, Jiang Xia Liu, Min Luo, Hang Su, Xiao-Zhong Fu*, Ting Liu, Yong-Xi Dong, Yong-Long Zhao, Bin He, Yong-Jun Li. Novel adefovir mono L-amino acid ester, mono bile acid ester derivatives: Design, synthesis, biological evaluation, and molecular docking study. Med Chem Res. 2017, 26, 1812-1821

4.Yu Ou, Min Luo, Yong-Xi Dong, Hang Su, Xiao-Zhong Fu*, Yu-Feng Cha,Shun Zhang, Yong-Long Zhao, Yong-Jun Li, Yong-Lin Wang.Permeability of novel 4′-N-substituted (aminomethyl) benzoate-7- substituted nicotinic acid ester derivatives of scutellarein in Caco-2 cells and in an invitro model of the blood-brain barrier. Med Chem Res. 2016, 25,2205-2213.

5.Yu-Feng Cha, Shun Zhang, Hang Su, Yu Ou, Xiao-Zhong Fu*, Feng-Jie Jiang,Yong-Long Zhao, Yong-Xi Dong, Min Luo, Yong Huang,Yan-Yu Lan, Ai-Min Wang, Yong-Lin Wang. L-Aminoacid carbamate prodrugs of scutellarin: synthesis, physiochemical property,Caco-2 cell permeability, and In Vivo anti-oxidative activity Med Chem Res. 2015, 24, 2238-2246.

6. Ze-Qin Dai, Hang Su, Min Luo, Yu Ou, Xiao-Zhong Fu*,Yu-Feng Cha, Shun Zhang, Yong Huang, Yong-Lin Wang. Applicationof N-substituted (aminomethyl) benzoate Strategy in Design of ScutellareinDerivatives with Improved Caco-2 Cell Permeability and In vitro AntioxidativeActivity Bull K Chem Soc 2015, 36,1959-1965.

7. Xiaozhong Fu*, FengjieJiang, Yu Ou, Sheng Fu, Yufeng Cha, Shun Zhang, Zongyuan Liu, Wen Zhou,Yonglin Wang* Synthesis and anti-HBV evaluation of mono L-amino acidester, mono non-steroid anti-inflammation drug carboxylic ester derivatives ofacyclonucleoside phosphonates. Chin Chem Lett 2014,25,115-118

7.FengjieJiang, Xiaozhong Fu*, Shanwu Wang, Yong Huang, Wen Zhou, Aimin Wang and Yonglin Wang*.Synthesis and physiochemical property evaluationof carbamate derivatives of scutellarin methyl ester Chin Chem Lett 2013, 24, 338-340

8.Xiao-Zhong Fu, Yu Ou,Jian-Ying Pei,Ying Liu, Jing Li, Wen Zhou, Yan-Yu Lan, Ai-Min Wang and Yong-Lin Wang *. Synthesis, anti-HBV activityand renal cell toxicity evaluation of mixed phosphonate prodrugs ofadefovir Eur J Med Chem 2012, 49,211-218.

9.Xiao Zhong Fu, Yu Ou, Jian Xin, Yu She Yang*. Design,synthesis and in vivo evaluation of mono (2,2,2- tri- fluoroethyl) esters, monoL-amino acid ester prodrugs of acyclic nucleoside phosphonates as anti-HBVagents Chin Chem Lett 2011, 22,1387-1390.

10.Xiao-ZhongFu, Feng-Jing Xing, Yan-Yu Lan, Ai-Min Wang, Yong-Lin Wang,* Jing Li, Wen Zhou, Wei Zhang, Ying Liu. Synthesis and in vitroanti-oxidative activity studies of 4’-N-substituted (amino methyl) benzoatederivativesof Scutellarein. Chin J Org Chem, 2011,31(7) : 1043-1048.

11.Xiao-Zhong Fu*, Ying Huang, Zhu Tao, Sai-Feng Xue, Chun Luo, Yu Ou, Jian-XinZhang. Investigation of Complex of Cucurbit[6, 7, 8]urils with AdefovirBis(L-amino acid) Ester Prodrug and Its Anti-HBV Activity. Chin J Org Chem 2010, 30 (5):675-683.

12. Xiaozhong Fu, SaihongJiang, Chuan Li, Jian Xin, Yushe Yang*, Ruyun Ji. Design and synthesis of novelbis(L-amino acid) ester prodrugs of 9-[2- (phosphono methoxy) ethyl] adenine(PMEA) with improved anti-HBV activity. Bioorg. Med Chem Lett 2007, 17(2): 465-470.

13.Xiaozhong Fu, Sai Hong Jiang, Jian Xin, Yushe Yang*. Design,synthesis and in vitro Evaluation of L-amino acid esters prodrugs of acyclicnucleoside phosphonates as anti-HBV agent. Chin Chem Lett 2007,18(7): 817-819.

14. Xiaozhong Fu, SaihongJiang, Peng Lu, Yushe Yang*, Ruyun Ji. An improved synthetic process for YF-6,A promising anti-HBV drug candidate. Org Prep Proced In 2008, 40 (5): 467-470.

15.Xiaozhong Fu, Sai Hong Jiang, Jian Xin, Yushe Yang*. Design,synthesis and in vitro Evaluation of L-amino acid esters prodrugs of acyclicnucleoside phosphonates as anti-HBV agent. Chin Chem Lett 2007,18(7): 817-819.

(二)会议论文

Xiao-Zhong Fu*, Yu Ou, Yong-Lin Wang, Design and synthesis of adefovir mixed phosphonate prodrugs with reduced renal cell toxicity by using human renal Organic Anion Transporter 1(hOAT1) as potential targets, BIT’3rd Annual Symposium of Drug Delivery System 2013,228,海口,2013.11.13-16,大会报告.

(三)获得奖励情况

1、傅晓钟,黄英,陶朱,薛赛凤,罗春,欧瑜,张建新.“Investigation of Complex of Cucurbit [6, 7, 8]urils with Adefovir Bis(L-amino acid)Ester Prodrug and Its Anti-HBV Activity,Chinese Journal ofOrganic Chemistry 2010, 5, 675-683 ”论文获得贵州省首届优秀医学学术论文三等奖,获奖时间2011年2月,授奖部门贵州省卫生厅、贵州省科教办。

2、傅晓钟贵州省第九批优秀青年科技人才培养对象,获奖时间2013 年4月,授奖部门贵州省优秀青年科技人才培养领导小组。

3、傅晓钟贵州省优秀教师,获奖时间2013 年9月,授奖部门贵州省教育厅,贵州省人力资源与社会保障厅。

(四)获得授权或申请发明专利情况

1、杨玉社,傅晓钟,李战,嵇汝运嘌呤类化合物双氨基酸酯的制备方法与用途授权时间2011.2.16,中国,专利授权号:ZL200610024401.6。

2、杨玉社,傅晓钟,李战,嵇汝运用于治疗乙型肝炎的嘌呤类化合物及其制备方法和用途授权时间2011.9.21,中国,专利授权号:ZL200610027328.8。

3、傅晓钟,兰燕宇,周雯,李勇军,欧瑜,王永林,王爱民,罗春,郑林,黄勇一类治疗乙型肝炎的嘌呤类衍生物、其制备方法与用途申请时间2009.11.20,中国,专利申请号:200910102876.6。

4、傅晓钟,兰燕宇,刘影,周雯,张伟,李勇军,李靖,王永林,王爱民,邢凤晶,郑林,黄勇治疗血管性痴呆的灯盏乙素苷元衍生物、其制备方法与用途申请时间2011.1.27 专利申请号:201010213663.3。

5、傅晓钟,王永林,姜凤洁,兰燕宇,李勇军,王爱民,黄勇,周雯,查雨锋,张顺,刘宗炎,欧瑜灯盏乙素及其苷元氨基甲酸酯衍生物及其应用申请时间 2013.10.10,中国,专利申请号:201310469734.X。


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