1-(substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors of Trypanosoma cruzi in mice. - Suppr | 超能文献

1-(substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors of Trypanosoma cruzi in mice.

作者信息

Chabala J C, Waits V B, Ikeler T, Patchett A A, Payne L, Peterson L H, Reamer R A, Hoogsteen K, Wyvratt M, Hanson W L

机构信息

Merck Sharp & Dohme Research Laboratories, Rahway, New Jersey 07065.

出版信息

Experientia. 1991 Jan 15;47(1):51-3. doi: 10.1007/BF02041250.

DOI:10.1007/BF02041250

Abstract

1-(Substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors of Trypanosoma cruzi infections in mice. The most active compounds are the 1-(4-chlorobenzyl)- and 1-(3,4-dichlorobenzyl)-analogs (L-153,094 [2] and L-153,153 [4], resp.) which are approximately 7-fold more potent upon oral administration than nifurtimox (Lampit) in suppressing parasite levels in the blood of mice with acute Trypanosoma cruzi infections.

摘要

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本文引用的文献

1

A new and convenient synthesis of 4-amino-5-imidazolecarboxamide.4-氨基-5-咪唑甲酰胺的一种新型便捷合成方法。

J Biol Chem. 1949 Nov;181(1):89-93.

2

Purines, pyrimidines, and imidazoles. XXXIX. Formation of some 5-aminoimidazole-4-carboxylic acid derivatives from ethyl -amino- -cyanoacetate.

J Chem Soc Perkin 1. 1972;13:1715-7. doi: 10.1039/p19720001715.

3

Density of parasites in various organs and the relation to numbers of trypomastigotes in the blood during acute infections of Trypanosoma cruzi in mice.小鼠急性克氏锥虫感染期间，各器官中寄生虫的密度及其与血液中锥鞭毛体数量的关系。

J Protozool. 1974 Oct;21(4):512-7. doi: 10.1111/j.1550-7408.1974.tb03689.x.

4

Immunization of mice with irradiated Trypanosoma cruzi growth in cell culture: relation of numbers of parasites, immunizing injections, and route of immunization to resistance.用细胞培养中经辐照的克氏锥虫对小鼠进行免疫：寄生虫数量、免疫注射次数以及免疫途径与抵抗力的关系。

Int J Parasitol. 1976 Aug;6(4):341-7. doi: 10.1016/0020-7519(76)90057-6.

5

In search of anti-Trypanosoma cruzi drugs: new leads from a mouse model.寻找抗克氏锥虫药物：来自小鼠模型的新线索。

J Med Chem. 1977 Jun;20(6):741-4. doi: 10.1021/jm00216a001.