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本文引用的文献

1
Polyamine synthesis and interconversion by the Microsporidian Encephalitozoon cuniculi.微小孢子虫兔脑炎微孢子虫的多胺合成与相互转化
J Eukaryot Microbiol. 2001 May-Jun;48(3):374-81. doi: 10.1111/j.1550-7408.2001.tb00327.x.
2
Polyamines with N-(3-phenylpropyl) substituents are effective competitive inhibitors of trypanothione reductase and trypanocidal agents.带有N-(3-苯丙基)取代基的多胺是有效的锥虫硫醇还原酶竞争性抑制剂和杀锥虫剂。
Bioorg Med Chem Lett. 2001 Jan 22;11(2):251-4. doi: 10.1016/s0960-894x(00)00643-0.
3
Terminally alkylated polyamine analogues as chemotherapeutic agents.作为化疗药物的末端烷基化多胺类似物。
J Med Chem. 2001 Jan 4;44(1):1-26. doi: 10.1021/jm000084m.
4
CD8+ CTLs are essential for protective immunity against Encephalitozoon cuniculi infection.CD8 + 细胞毒性T淋巴细胞对于抵抗兔脑炎微孢子虫感染的保护性免疫至关重要。
J Immunol. 1999 May 15;162(10):6086-91.
5
TNP-470 is an effective antimicrosporidial agent.TNP - 470是一种有效的抗微孢子虫剂。
J Infect Dis. 1998 Feb;177(2):515-8. doi: 10.1086/517390.
6
Trypanosoma brucei: lack of cross-resistance to melarsoprol in vitro by cymelarsan-resistant parasites.布氏锥虫：抗环美胂寄生虫在体外对美拉胂醇不存在交叉耐药性。
Exp Parasitol. 1997 Jul;86(3):181-90. doi: 10.1006/expr.1997.4167.
7
Polyamine metabolism as a therapeutic target for Microsporidia.多胺代谢作为微孢子虫的治疗靶点。
J Eukaryot Microbiol. 1996 Sep-Oct;43(5):96S. doi: 10.1111/j.1550-7408.1996.tb05020.x.
8
Preparation of the pure diastereomeric forms of S-(5'-deoxy-5'-adenosyl)-1-ammonio-4-methylsulfonio-2-cyclopentene and their evaluation as irreversible inhibitors of S-adenosylmethionine decarboxylase from Escherichia coli.S-(5'-脱氧-5'-腺苷基)-1-铵基-4-甲基硫代-2-环戊烯纯非对映体形式的制备及其作为大肠杆菌S-腺苷甲硫氨酸脱羧酶不可逆抑制剂的评价。
Bioorg Med Chem. 1993 Nov;1(5):349-60. doi: 10.1016/s0968-0896(00)82141-0.
9
Experimental microsporidiosis in immunocompetent and immunodeficient mice and monkeys.免疫功能正常和免疫功能低下的小鼠及猴子的实验性微孢子虫病
Folia Parasitol (Praha). 1994;41(1):1-11.
10
S-(5'-deoxy-5'-adenosyl)-1-aminoxy-4-(methylsulfonio)-2-cyclopentene (AdoMao): an irreversible inhibitor of S-adenosylmethionine decarboxylase with potent in vitro antitrypanosomal activity.S-（5'-脱氧-5'-腺苷基）-1-氨氧基-4-（甲基硫代）-2-环戊烯（AdoMao）：一种S-腺苷甲硫氨酸脱羧酶的不可逆抑制剂，具有强大的体外抗锥虫活性。
J Med Chem. 1995 May 12;38(10):1770-7. doi: 10.1021/jm00010a021.

具有抗锥虫和抗微孢子虫活性的新型烷基多胺类似物。

Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity.

作者信息

Zou Y, Wu Z, Sirisoma N, Woster P M, Casero R A, Weiss L M, Rattendi D, Lane S, Bacchi C J

机构信息

Department of Pharmaceutical Sciences, Wayne State University, Detroit, MI 48202, USA.

出版信息

Bioorg Med Chem Lett. 2001 Jun 18;11(12):1613-7. doi: 10.1016/s0960-894x(01)00315-8.

DOI:10.1016/s0960-894x(01)00315-8
PMID:11412992
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3109676/
Abstract

A novel series of alkyl- or aralkyl-substituted polyamine analogues was synthesized containing a 3-7-3 polyamine backbone. These analogues were evaluated in vitro, and in one case in vivo, for activity as antitrypanosomal agents, and for activity against opportunistic infection caused by Microsporidia. Compound 21 inhibits trypanosomal growth with an IC(50) as low as 31nM, while compound 24 shows promising activity in vitro against trypanosomes, and against Microsporidia in vitro and in vivo.

摘要

合成了一系列新型的含有3-7-3多胺主链的烷基或芳烷基取代的多胺类似物。对这些类似物进行了体外评估，并且在一个案例中进行了体内评估，以检测其作为抗锥虫剂的活性以及针对由微孢子虫引起的机会性感染的活性。化合物21抑制锥虫生长，其半数抑制浓度（IC50）低至31 nM，而化合物24在体外对锥虫以及在体外和体内对微孢子虫均显示出有前景的活性。