抗感染药物研究进展
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摘要
抗感染药物临床应用十分广泛。以我国学者2010 2011年在国内外发表的论文为素材,总结了我国抗感染药物的研究进展,主要包括活性较好且结构新颖的抗菌新药、抗病毒新药和抗真菌新药的发现,以及莫西沙星和利奈唑胺等抗菌药物的合成工艺改进。
Anti-infective agents have a wide range of clinical applications.Based on the publications of the Chinese scientists during 2010-2011,this review summarized the domestic development of antiinfective agents in the following aspects: new drug discovery of novel antibacterials,antivirals,and antifungals with good activities as well as the process improvement on some antibacterials such as moxifloxacin and linezolid.
Anti-infective agents have a wide range of clinical applications.Based on the publications of the Chinese scientists during 2010-2011,this review summarized the domestic development of antiinfective agents in the following aspects: new drug discovery of novel antibacterials,antivirals,and antifungals with good activities as well as the process improvement on some antibacterials such as moxifloxacin and linezolid.
引文
[1]万志龙,柴芸,刘明亮,等.7-(3-甲基-3-甲氨基-4-烷氧亚胺基-1-哌啶基)喹诺酮类化合物的合成和体外抗菌作用[J].药学学报,2010,45(7):860-868.
[2]郭强,冯连顺,刘明亮,等.7-(3-胺甲基-4-(脲亚氨基)吡咯烷-1-基)喹诺酮衍生物的合成和抗菌作用研究[J].中国抗生素杂志,2011,36(6):434-440.
[3]Zhang Y B,Li G Q,Liu M L,et al.Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-5-amino/methylaminopiperidin-1-yl)fluoroquinolone derivatives[J].Bioorg Med Chem Lett,2011,21(3):928-931.
[4]Chai Y,Wang J,Liu M L,et al.Design,synthesis and in vitro antibacterial activity of 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl)fluoroquinolone derivatives[J].Bioorg Med Chem Lett,2011,21(11):3377-3380.
[5]Chai Y,Liu M L,Wang B,et al.Synthesis and in vitro antibacterial activity of novel fluoroquinolone derivatives containing substituted piperidines[J].Bioorg Med Chem Lett,2010,20(17):5195-5198.
[6]Xin Q S,Fan H X,Guo B,et al.Design,synthesis and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents[J].J Med Chem,2011,54(21):7493-7502.
[7]Shao C,Zhou W C,Zhang S L,et al.Synthesis and antibacterial activity of N4-mono alkyl derivatives of novel glycopeptide LYV07ww01[J].Bioorg Med Chem Lett,2011,21(22):6732-6738.
[8]Xu P,Chen X Z,Liu L,et al.A new series of macrolide derivatives with 4″-O-saccharide substituents[J].Bioorg Med Chem Lett,2010,20(18):5527-5531.
[9]Yu L L,Zhou W C,Wang Z Y.Synthesis and in vitro antibacterial activity of oxazolidine LBM-415 analogs as peptide deformylase inhibitors[J].Bioorg Med Chem Lett,2011,21(5):1541-1544.
[10]Shi W,Duan Y Q,Qian Y,et al.Design,synthesis and antibacterial activity of 2,5-dihydropyrrole formylhydroxyamino derivatives as novel peptide deformylase inhibitors[J].Bioorg Med Chem Lett,2010,20(12):3592-3595.
[11]Shi W,Ma H K,Duan Y Q,et al.Design,synthesis and antibacterial activity of 3-methylenepyrrolidine formylhydroxyamino derivatives as novel peptide deformylase inhibitors[J].Bioorg Med Chem Lett,2011,21(3):1060-1063.
[12]仇记宽,刘国生,李建平,等.新型含吡唑基的α-氨基磷酸酯类衍生物的合成和生物活性[J].有机化学,2011,31(1):63-67.
[13]夏庆春,何其庄,许东方,等.吡唑三杂环化合物的制备表征及生物活性的研究[J].化学学报,2010,68(23):2414-2420.
[14]陈华,谷云景,苑香果,等.含嘧啶胺基的三取代三嗪衍生物的合成及其抗菌、抗肿瘤活性研究[J].有机化学,2011,31(8):1266-1271.
[15]Zhang F F,Gan L L,Zhou C H.Synthesis antibacterial and antifungal activities of some carbazole derivatives[J].Bioorg Med Chem Lett,2010,20(6):1881-1884.
[16]Zhang Y Y,Zhou C H.Synthesis and activity of naphthali-mide azoles as a new type of antibacterial and antifungalagents[J].Bioorg Med Chem Lett,2011,21(14):4349-4352.
[17]Li H Q,Luo Y,Zhu H L.Discovery of vinylogous carba-mates as a novel class ofβ-ketoacyl-acyl carrier proteinsynthase III(FabH)inhibitors[J].Bioorg Med Chem,2011,19(15):4454-4459.
[18]Cheng K,Zheng Q Z,Hou J,et al.Synthesis,molecularmodeling and biological evaluation of PSB as targeted an-tibiotics[J].Bioorg Med Chem,2010,18(7):2447-2455.
[19]Li H Q,Luo Y,Lv P C,et al.Design and synthesis of no-vel deoxybenzoin derivatives as FabH inhibitors and anti-inflammatory agents[J].Bioorg Med Chem Lett,2010,20(6):2025-2028.
[20]Xiao Z P,Yang H O,Wang X D,et al.4-Alkoxy-3-arylfu-ran-2(5H)-ones as inhibitors of tyrosyl-tRNA synthetase:synthesis,molecular docking and antibacterial evaluation[J].Bioorg Med Chem,2011,19(13):3884-3891.
[21]程青芳,王启发,许兴友,等.莫西沙星的合成[J].中国医药工业杂志,2010,41(8):561-563.
[22]刘巧云,陈文华,郭亮.2,6-二氯-5-氟烟酰乙酸乙酯的合成[J].中国医药工业杂志,2010,41(8):571-572.
[23]张慧,杜鲲,桑志培,等.利奈唑胺的合成[J].中国医药工业杂志,2011,42(4):245-247.
[24]卢庆梁,周金培.氟苯考尼的合成[J].中国医药工业杂志,2010,41(7):481-484.
[25]李春鑫,山广志,樊博,等.格尔德霉素衍生物TC-GM的合成及体外抗病毒活性研究[J].药学学报,2011,46(6):683-687.
[26]郭会芳,李玉环,陶佩珍,等.环己酰亚胺及其衍生物的抗病毒活性研究[J].药学学报,2010,45(2):268-273.
[27]张烁,曹眸,关注,等.异核苷及其单磷酸酯的合成和抗病毒活性研究[J].中国药物化学杂志,2011,21(2):96-105.
[28]赵芡,卢俊瑞,辛春伟,等.1-(4-取代苯基)-4-苯基-5-(2-羟基苄基)氨基-1,2,3-三唑类衍生物的合成和抑菌活性[J].高等学校化学学报,2011,32(12):2806-2811.
[29]朱姗姗,卢俊瑞,辛春伟,等.3-取代硫基-5-(1-羟基苯基)-4H-1,2,4-三唑类化合物的合成和抑菌活性[J].高等学校化学学报,2010,31(11):2228-2233.
[30]Jiang Y W,Zhang J,Cao Y B,et al.Synthesis,in vitroevaluation and molecular docking studies of new triazolederivatives as antifungal agents[J].Bioorg Med ChemLett,2011,21(15):4471-4475.
[31]Chai X Y,Zhang J,Cao Y B,et al.New azoles with anti-fungal activity:design,synthesis,and molecular docking[J].Bioorg Med Chem Lett,2011,21(2):686-689.
[32]Liu Y,Liu Z N,Cao X F,et al.Design and synthesis ofpyridine-substituted itraconazole analogues with improvedantifungal activities,water solubility and bioavailability[J].Bioorg Med Chem Lett,2011,21(16):4779-4783.
[2]郭强,冯连顺,刘明亮,等.7-(3-胺甲基-4-(脲亚氨基)吡咯烷-1-基)喹诺酮衍生物的合成和抗菌作用研究[J].中国抗生素杂志,2011,36(6):434-440.
[3]Zhang Y B,Li G Q,Liu M L,et al.Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-5-amino/methylaminopiperidin-1-yl)fluoroquinolone derivatives[J].Bioorg Med Chem Lett,2011,21(3):928-931.
[4]Chai Y,Wang J,Liu M L,et al.Design,synthesis and in vitro antibacterial activity of 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl)fluoroquinolone derivatives[J].Bioorg Med Chem Lett,2011,21(11):3377-3380.
[5]Chai Y,Liu M L,Wang B,et al.Synthesis and in vitro antibacterial activity of novel fluoroquinolone derivatives containing substituted piperidines[J].Bioorg Med Chem Lett,2010,20(17):5195-5198.
[6]Xin Q S,Fan H X,Guo B,et al.Design,synthesis and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents[J].J Med Chem,2011,54(21):7493-7502.
[7]Shao C,Zhou W C,Zhang S L,et al.Synthesis and antibacterial activity of N4-mono alkyl derivatives of novel glycopeptide LYV07ww01[J].Bioorg Med Chem Lett,2011,21(22):6732-6738.
[8]Xu P,Chen X Z,Liu L,et al.A new series of macrolide derivatives with 4″-O-saccharide substituents[J].Bioorg Med Chem Lett,2010,20(18):5527-5531.
[9]Yu L L,Zhou W C,Wang Z Y.Synthesis and in vitro antibacterial activity of oxazolidine LBM-415 analogs as peptide deformylase inhibitors[J].Bioorg Med Chem Lett,2011,21(5):1541-1544.
[10]Shi W,Duan Y Q,Qian Y,et al.Design,synthesis and antibacterial activity of 2,5-dihydropyrrole formylhydroxyamino derivatives as novel peptide deformylase inhibitors[J].Bioorg Med Chem Lett,2010,20(12):3592-3595.
[11]Shi W,Ma H K,Duan Y Q,et al.Design,synthesis and antibacterial activity of 3-methylenepyrrolidine formylhydroxyamino derivatives as novel peptide deformylase inhibitors[J].Bioorg Med Chem Lett,2011,21(3):1060-1063.
[12]仇记宽,刘国生,李建平,等.新型含吡唑基的α-氨基磷酸酯类衍生物的合成和生物活性[J].有机化学,2011,31(1):63-67.
[13]夏庆春,何其庄,许东方,等.吡唑三杂环化合物的制备表征及生物活性的研究[J].化学学报,2010,68(23):2414-2420.
[14]陈华,谷云景,苑香果,等.含嘧啶胺基的三取代三嗪衍生物的合成及其抗菌、抗肿瘤活性研究[J].有机化学,2011,31(8):1266-1271.
[15]Zhang F F,Gan L L,Zhou C H.Synthesis antibacterial and antifungal activities of some carbazole derivatives[J].Bioorg Med Chem Lett,2010,20(6):1881-1884.
[16]Zhang Y Y,Zhou C H.Synthesis and activity of naphthali-mide azoles as a new type of antibacterial and antifungalagents[J].Bioorg Med Chem Lett,2011,21(14):4349-4352.
[17]Li H Q,Luo Y,Zhu H L.Discovery of vinylogous carba-mates as a novel class ofβ-ketoacyl-acyl carrier proteinsynthase III(FabH)inhibitors[J].Bioorg Med Chem,2011,19(15):4454-4459.
[18]Cheng K,Zheng Q Z,Hou J,et al.Synthesis,molecularmodeling and biological evaluation of PSB as targeted an-tibiotics[J].Bioorg Med Chem,2010,18(7):2447-2455.
[19]Li H Q,Luo Y,Lv P C,et al.Design and synthesis of no-vel deoxybenzoin derivatives as FabH inhibitors and anti-inflammatory agents[J].Bioorg Med Chem Lett,2010,20(6):2025-2028.
[20]Xiao Z P,Yang H O,Wang X D,et al.4-Alkoxy-3-arylfu-ran-2(5H)-ones as inhibitors of tyrosyl-tRNA synthetase:synthesis,molecular docking and antibacterial evaluation[J].Bioorg Med Chem,2011,19(13):3884-3891.
[21]程青芳,王启发,许兴友,等.莫西沙星的合成[J].中国医药工业杂志,2010,41(8):561-563.
[22]刘巧云,陈文华,郭亮.2,6-二氯-5-氟烟酰乙酸乙酯的合成[J].中国医药工业杂志,2010,41(8):571-572.
[23]张慧,杜鲲,桑志培,等.利奈唑胺的合成[J].中国医药工业杂志,2011,42(4):245-247.
[24]卢庆梁,周金培.氟苯考尼的合成[J].中国医药工业杂志,2010,41(7):481-484.
[25]李春鑫,山广志,樊博,等.格尔德霉素衍生物TC-GM的合成及体外抗病毒活性研究[J].药学学报,2011,46(6):683-687.
[26]郭会芳,李玉环,陶佩珍,等.环己酰亚胺及其衍生物的抗病毒活性研究[J].药学学报,2010,45(2):268-273.
[27]张烁,曹眸,关注,等.异核苷及其单磷酸酯的合成和抗病毒活性研究[J].中国药物化学杂志,2011,21(2):96-105.
[28]赵芡,卢俊瑞,辛春伟,等.1-(4-取代苯基)-4-苯基-5-(2-羟基苄基)氨基-1,2,3-三唑类衍生物的合成和抑菌活性[J].高等学校化学学报,2011,32(12):2806-2811.
[29]朱姗姗,卢俊瑞,辛春伟,等.3-取代硫基-5-(1-羟基苯基)-4H-1,2,4-三唑类化合物的合成和抑菌活性[J].高等学校化学学报,2010,31(11):2228-2233.
[30]Jiang Y W,Zhang J,Cao Y B,et al.Synthesis,in vitroevaluation and molecular docking studies of new triazolederivatives as antifungal agents[J].Bioorg Med ChemLett,2011,21(15):4471-4475.
[31]Chai X Y,Zhang J,Cao Y B,et al.New azoles with anti-fungal activity:design,synthesis,and molecular docking[J].Bioorg Med Chem Lett,2011,21(2):686-689.
[32]Liu Y,Liu Z N,Cao X F,et al.Design and synthesis ofpyridine-substituted itraconazole analogues with improvedantifungal activities,water solubility and bioavailability[J].Bioorg Med Chem Lett,2011,21(16):4779-4783.