药物代谢研究与药物设计及结构修饰
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to poiso meraseⅡmediated DN A cleavag e by a pro to ber berine alkaloid,ber berr ubine[J].
Biochemistry,1998,37:16316-16324.
[2]Elfo rd B C.L-G lutamine influx in mala ria-infected
er ythr ocy tes:a tar get fo r antimalarials[J].Parasitol Today,1986,2(11):309-312.
[3]Jo nathan L V;Daniel K.Pr oto berberine a lkaloids as
antima la rials[J].J Med Chem,1988,31(6):1085-1087.
[4]Iwasa K,Kim H y e-So ok,W ataya Y,e t a l.
Antimalarial activity and structure-activity r ela tio nships o f pr o to berberine alkalo ids[J].Eur J Med Chem,1998,33:65-69.
[5]Bo rdo r N,Brew ster M E.Im pr ov ed deliv ery th rough
bio lo gica l membranes——sustained brain deliv e ry o f ber berine[J].Eur J Med Chem,1983,18:235-240. [6]Iw asa K,Nishiya ma Y,Ichima ru M,et al.Structure-
activ ity r ela tionships of qua ter nar y pr oto berberine alkaloids having antimala rial activity[J].Eur J Med Chem,1999,,34:1077-1083.
[7]季宇彬.中草药有效成分药理与其应用[M].哈尔滨:
黑龙江科学技术出版社,1994.69-80.
[8]Iwa sa K,Kamiga uchi M,U eki M,et al.Structure-
activ ity r elationships o f ber be rine analo gs[J].Eur J Med Chem,1996,31:469-478.
[9]Iw asa K,Ka mig uauchi M,Sug lura M,et a l.
Antimic ro bia l activity of some13-alkayl-substituted pro to ber berinium salts[J].Planta Med,1997,63:
196-198.
[10]Iw asa K,Na nba H,Lee Dong-U ng,et al.Str uc ture-
activity relatio nships of pro to be rberines having
antimic robia l activity[J].Planta Med,1998,64:748-751.
[11]Iw asa K,Lee Dong-U ng,Kang So-Im,e t al.
Antimicr obial activ ity o f8-alkay l-and8-phenyl-substituted be rberines a nd th eir12-br omo deriv a tiv es
[J].J N at Prod,1998,61(9):1150-1153.
[12]Ho ng S W,Kim S H,J eun J A,et a l.Antimicr obial
activity of9-O-acyl-and9-O-be nzoy l-substituted
berber rubines[J].Planta Med,2000,66:361-363. [13]翁尊尧,王肇瀛,业晓明.抗肿瘤物质——恩其明
(U N GERM IN G,A T-1840)及其有关化合物的合成和构效关系[J].药学学报,1982,10:744-748.
[14]M anohar L S.Enzy me inhibitionⅥ:inhibitio n of
rev erse tr anscriptase ac tiv ity by pro tober be rine alkaloids and structure-a ctivity relatio nships[J].J
Pharm Sci,1983,72(5):538-541.
[15]林菁.小檗碱对K562细胞生长的抑制作用[J].福建
医学学报,1996,30:309-312.
[16]Ko bayashi Y,Yamashita Y,Fujii N,et al.Inhibito rs
of DN A to po iso meraseⅠandⅡisolated f rom the coptis rhizo mes[J].Planta Me d,1995,61:414-418. [17]Sch mekker T,Lat z-Br uning B,W ink M.B iochemical
activities o f ber berine,palmatine and sang uina rine mediating chmical defence ag ainst micr oog anisms and
herbiv or es[J].Phytochemistry,1997,44(2):257-266.
药物代谢研究与药物设计及结构修饰
阿基业, 王广基
(中国药科大学药代中心,南京210009)
摘 要:药物代谢研究可以为药物设计及结构修饰提供帮助和指导。阐述药物代谢研究与药物设计及结构修饰的密切联系,介绍药物代谢和活性代谢产物研究在前体药物设计、化合物结构改造或引入合适基团及硬药和软药开发等方面的作用。
关键词:药物代谢;前体药物;代谢产物;药物设计;结构修饰
中图分类号:R969.1;R914.2 文献标识码:A 文章编号:1001-5094(2002)02-080-07
Drug Metabolism Research for the Design and Structural Modification of Drugs
A J i-ye, W AN G Guang-ji
(Center of Metabolism and Pharmacokinetics,China Pharmaceutical University,N anjing210009,China)接受日期:2002-02-02