中國藥科大學(xué)藥學(xué)院導(dǎo)師:徐進(jìn)宜

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中國藥科大學(xué)藥學(xué)院導(dǎo)師:徐進(jìn)宜

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中國藥科大學(xué)藥學(xué)院導(dǎo)師:徐進(jìn)宜 正文


  個人情況簡介
  徐進(jìn)宜,教授,博導(dǎo),藥學(xué)院藥物化學(xué)教研室副主任。

  主要研究方向
 ?。?)心血管新藥分子的設(shè)計與合成研究;(2)天然活性產(chǎn)物的結(jié)構(gòu)修飾、半合成及生物活性研究。

  擔(dān)任國家863計劃評審專家、國家自然科學(xué)基金評審專家和農(nóng)業(yè)部獸藥審評專家;擔(dān)任Journal of Medicinal Chemistry, Current Medicinal Chemistry,European Journal of Medicinal Chemistry, Bioorganic & Medicinal Chemistry 等雜志特邀審稿人。

  研究經(jīng)歷包括:
  非肽類血管緊張素II受體拮抗劑的設(shè)計與合成研究;AT1受體拮抗劑類新藥氯沙坦、依貝沙坦、坎地沙坦的合成工藝研究;血管緊張素AT1受體和內(nèi)皮素ETA受體雙重拮抗劑的研究;新型抗高血壓藥物及抗心衰藥物的研究;新型α1-受體阻斷劑及鈣拮抗劑的研究;選擇性環(huán)氧化酶II抑制劑的研究;非苯二氮卓類GABAA受體激動劑的研究;COX-2/5-LOX雙重抑制劑的研究;23-羥基白樺酸的結(jié)構(gòu)改造與生物活性研究;喜樹堿的結(jié)構(gòu)修飾與生物活性研究;天然活性產(chǎn)物XJP的全合成及其類似物的設(shè)計合成研究;冬凌草甲素的結(jié)構(gòu)修飾與生物活性研究;手性O(shè)cotillol型人參皂苷衍生物的設(shè)計合成研究;在日本近畿大學(xué)完成了天然活性產(chǎn)物Gregatin B的全合成研究。

  近年主持研究項目包括:
  “重大新藥創(chuàng)制”國家重大科技專項:一類抗高血壓新藥ATPT的研究(化學(xué)藥品注冊分類Ⅰ)(2009ZX09102-036);國家自然科學(xué)基金面上項目:新血管緊張素II受體拮抗劑的設(shè)計、合成及生物活性研究(No. 30371688);國家自然科學(xué)基金面上項目:以天然活性產(chǎn)物冬凌草甲素結(jié)構(gòu)為模板的創(chuàng)新藥物分子設(shè)計與評價的探索研究(30973610);教育部科學(xué)技術(shù)研究重點(diǎn)項目:冬凌草甲素的結(jié)構(gòu)改造與生物活性研究(108069);江蘇省自然科學(xué)基金項目:新型非甾體抗炎藥COX-2抑制劑的研究(BK2004109);江蘇省自然科學(xué)基金項目:新型AT1/ETA雙重受體拮抗劑的設(shè)計合成、生物活性及其構(gòu)效關(guān)系研究(BK2008344)。作為第一參加者參與了江蘇省醫(yī)藥科技攻關(guān)項目:抗高血壓新藥ATPT的研究(BG2006610);國家自然科學(xué)基金面上項目:天然產(chǎn)物 23-羥基白樺酸的結(jié)構(gòu)改造與生物活性研究(30472083);國家自然科學(xué)基金面上項目:天然產(chǎn)物XJP及其類似物的合成、生物活性及其構(gòu)效關(guān)系研究(30873144);重大新藥創(chuàng)制”國家重大科技專項:抗高血壓候選藥物XJP的研究(化學(xué)藥品注冊分類Ⅰ)(2009ZX09103-128)。

  在國內(nèi)外期刊發(fā)表論文80余篇,其中SCI論文40余篇;申請國內(nèi)外發(fā)明專利20項,參編著作9部。指導(dǎo)博士研究生、碩士研究生共32名,榮獲教書育人優(yōu)秀教師獎。

  近期代表性論文和著作
  (1)  Jinyi Xu, Yi Zeng, Xiao Ming WU, et al. Synthesis and biological activity of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety as novel angiotensin II AT1 receptor antagonists. Bioorg. & Med. Chem. Lett., 2007, 17 (10): 2921-2926.
  (2)  Jinyi Xu, Qian RAN, Xiao Ming WU, et al. Design and Synthesis of 2-Alkylbenzimidazole Derivatives as Novel Non-peptide Angiotensin II AT1 Receptor Antagonists. Chin. Chem. Lett., 2007, 18: 251-254.
  (3)  Yi Bi, Jinyi Xu*, Xiaoming Wu et al. Synthesis and Cytotoxic activity of 17-Carboxylic Acid Modified 23-Hydroxy Betulinic Acid Ester Derivatives. Bioorg. & Med. Chem. Lett., 2007, 17(5): 1475-1478.
  (4)  Yi Bi, Jinyi Xu*, Xiaoming Wu et al. Synthesis and Anti-tumor Activity of 30- Hydroxy Derivative s of -Hydroxy Betulinic Acid. J. Chin. Pharm. Univ., 2007, 38 (2): 108-111.
  (5)  Qian Ran, Jinyi Xu*, Xiao Ming Wu, et al. Advances in the research of Oridonin. Pharm. Clin. Res,2007, 15(2): 91-95.
  (6)  Zhen Wei, Jinyi Xu*, Xiao Ming Wu, et al. Development of Novel Dual Angiotesin II and Endothelin Receptor Antagonists. Progress. Pharm. Sci., 2006, 30(5): 193-197.
  (7)  Yi Zeng, Jinyi Xu*, Xiao Ming Wu, et al. The advances in R&D of selective COX-2 inhibitors. Chin. J. New Drug, 2006, 15(6), 410-415.
  (8)  Jinyi Xu, Qianhui He, Xiao Ming Wu, et al. Synthesis and Biological Activities of 4-Substituted-5-Alky-2,4-Dihydro-2-[3-Chloride-4-Fluorophenyl]-3H-1,2,4-Triazol-3-one Derive-
  rivatives. Chin. J. Org. Chem., 2006, 26(1): 123-128.
  (9)  Jinyi Xu, Hequan Yao, Xiaoming Wu. et al. Synthesis and Anti-inflammatory Activities of Diaryl-Substituted-1,2,4-Trizole Derivatives. J. Chem. Chin. Univ., 2005, 26(12): 2254-2258.
  (10) Jinyi Xu, Xiaoming Wu. Hua Wei-yi, et al. Synthesis of 5-Amido-1H-imidazo [5,4-b] pyridine Derivatives and their AngiotensinⅡ Receptor Antagonistic Activities. J. Chem. Chin. Univ., 2005, 26(6): 1067-1071.
  (11) Matsuo K, Kanayama M, Jinyi Xu, et al. Concise Formal Synthesis of (S)-Gregatin B. Heterocycles, 2005, 65(7): 1609-1614.
  (12) Jinyi Xu, Nianning Ji, Xiaoming Wu, et al. QSAR Studies of AngiotensinⅡAT1 Receptor Antagonists. J. Chin. Pharm. Univ., 2005, 36(2): 99-105.
  (13) Jinyi Xu, Wu Xiao-ming, Hua Wei-yi, et al. 4/-[(Triazolinone-1-yl) methyl] biphenyl- 2-sulfonamides Derivatives as Dual AngiotensinⅡ/ Endothelin A Receptor Antagonists. Drugs Fut., 2004, 29(Suppl. A): 266-267.
  (14) Jinyi Yang, Jinyi Xu*, Xiao Ming Wu, et al. Research on the Anti-tumor Natural Products.
  Chin. J. Mod. Appl. Pharm., 2007, 24(4): 277-282.
  (15) Bo Jiang, Jinyi Xu*, Xiao Ming Wu, et al. Advances in the Research on the Dual Cyclooxygenase-2(COX-2) and 5-Lipoxygenase (5-LOX) Inhibitors. Chin. J. Mod. Appl. Pharm., 2008, 25(2): 109-114.
  (16) Jinyi Xu*, Jingyi Yang, Qian Ran, Xiaoming Wu. et al. Synthesis and biological evaluation of novel 1-O- and 14-O-derivatives of oridonin as potential anticancer drug candidates. Bioorg. & Med. Chem. Lett., 2008, 18: 4741-4744.
  (17) Li Zhi Fu, Jinyi Xu*, He Quan Yao and Xiao Ming Wu. A synthesis of 4H-1, 4-benzothiazines. J. Chem. Res., 2008, (10): 566–567.
  (18) Jinyi Xu, Bo Jiang, Xiao Ming Wu, et al. Synthesis,anti-inflammatory activities and SAR studies of 1, 5-diarylsubstitued-1, 2, 4-trizoles. Chin. J. Med. Chem. 2008, 18(5), 321-328.
  (19) Diliang Guo, Jinyi Xu, Hualiang Jiang, and Hong Liu. Efficient Iron-Catalyzed N-Arylation of Aryl Halides with Amines. Organic Letters, 2008, 10, 4513-4516.
  (20) Bei Yan, Guangji Wang, Xiaoming Wu, Jinyi Xu, et al. Identification of the major metabolites of 1-(2,6-dichlorophenyl)-3-n-butyl-1,4-dihydro-4-{4-[2-(1H-tetrazole-5-yl)-1H- pyrrol-1-yl]phenylmethyl}-5H-1,2,4-triazol-5-one, a newangiotensin type 1 receptor antagonist, in rat bile by HPLC-diode array detection-MS and HPLC-MS/MS. Biomed. Chromatog., 2007, 21: 912-924.
  (21) Bei Yan, Guangji Wang, Xiaoming Wu, Jinyi Xu, et al. Determination of 1-(2,6-dichloro- phenyl)-3-n-butyl-1,4-dihydro-4-{4-[2-(1H-tetrazole-5-yl)-1H-pyrrol-1-yl]phenylmethyl}-5H-1,2,4-triazol-5-one, a newangiotensin type 1 receptor antagonist in rat plasma by LC-ESI-MS: Application to pharmacokinetic studies. Chromatographia, 2007, 66: 55-61.
  (22) Yu Wang, Qiujuan Wang, Jinyi Xu, et al. [Ca2+]i and PKC-a are involved in the inhibitory effects of Ib, a novel nonpeptide AngiotensinII subtype AT1 receptor antagonist, on AngiotensinII-induced vascular contraction in vitro. Biochemical and Biophysical Research Communications, 2007,364:118-123.
  (23) Jie Liu, Jinyi Xu *, Xiaoming Wu. et al. Total synthesis and antihypertensive activity of 7, 8-dihydroxy-3-methyl-isochromanone-4. Bioorg. & Med. Chem. Lett., 2009, 19: 1822-1824.
  (24) Peiqing Zhu, Yi Bi, Jinyi Xu *, Xiaoming Wu. et al. Terpenoids. III: Synthesis and biological evaluation of 23-hydroxybetulinic acid derivatives as novel inhibitors of glycogen phosphorylase. Bioorg. & Med. Chem. Lett., 2009, 19: 6966–6969.
  (25) Bo Jiang, Yi Zeng, Jinyi Xu *, Xiaoming Wu. et al. Design, Synthesis, and Biological Evaluation of 1, 5-Diarylsubstitued-1, 2, 4-triazole Derivatives as Selective Cyclooxygenase-2 Inhibitors. Archiv der Pharmazie, 2010, 9:500-508.
  (26) Diliang Guo, Jinyi Xu, Hong Liu, et al. Ligand-free Iron/Copper Cocatalyzed N-Arylations of Aryl Halides with Amines under Microwave Irradiation. Green Chemistry., 2010, 12, 276–281.
  (27) Yue Huang, Jinyi Xu, Xiaoming Wu, Hequan Yao. et al. Oxidation of 4-carboxylate
  thiazolines to 4-carboxylate thiazoles by molecular oxygen. Tetrahedron Letters. 2010,
  51:1751–1753.
  (28) Bingfeng Sun, Chaolei Wang, Jinyi Xu, Guoqiang Lin. Concise Approach to the Core of Englerin A via an Organocatalytic [4+3] Cycloaddition Reaction. Tetrahedron. Lett., 2011, 52, 2155-2158.
  (29) Lei Wang, Dahong Li, Jinyi Xu *. et al. Recent Progress in the Development of Natural ent-Kaurene Diterpenoids with Anti-tumor Activity. Mini-Reviews in Medicinal Chemistry 2011, 11: 41-48.
  (30) Wang Lei, Ran Qian, Li Dahong, Jinyi Xu *. et al. Synthesis and Biological Evaluation of 14-O-Derivatives of Natural Oridonin. Chin. J. Nat. Med., 2011, 9(3): 194-198.

  著作
 ?。?)主編《藥物化學(xué)》2006年6月, 化學(xué)工業(yè)出版社
 ?。?)參編《藥物化學(xué)》2004年10月,化學(xué)工業(yè)出版社
  (3)參編《藥物化學(xué)》2005年2月, 科學(xué)技術(shù)文獻(xiàn)出版社
 ?。?)參編《藥物化學(xué)實(shí)驗(yàn)指導(dǎo)》2000年3月,醫(yī)藥科技出版社
 ?。?)參編《藥物化學(xué)》2006年12月,東南大學(xué)出版社
 ?。?)參編《藥物化學(xué)》2006年12月,化學(xué)工業(yè)出版社
 ?。?)參編《藥物化學(xué)》2008年10月,東南大學(xué)出版社
 ?。?)參編《藥物化學(xué)雙語教學(xué)實(shí)驗(yàn)指導(dǎo)》2008年7月,醫(yī)藥科技出版社
 ?。?)參編《藥物化學(xué)進(jìn)展》2010年12月,化學(xué)工業(yè)出版社      

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