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2,2'-二氨基甲酰氧基-5,5'-二苯并咪唑基甲酮——一种新型抗丝虫药。

2,2'-Dicarbomethoxyamino-5,5'-dibenzimidazolyl ketone--a new antifilarial agent.

作者信息

Fatma N, Sharma S, Chatterjee R K

机构信息

Division of Parasitology, Central Drug Research Institute, Lucknow, India.

出版信息

Acta Trop. 1989 Oct;46(5-6):311-21. doi: 10.1016/0001-706x(89)90044-2.

Abstract

The activity of 2,2'-dicarbomethoxyamino-5,5'-dibenzimidazolyl ketone (II, C.D.R.I. Comp. 82/437) has been evaluated for its micro- and macro-filaricidal efficacy against Litomosoides carinii in rodents. A dose of 3 mg/kg (i.p.) and 50 mg/kg (oral) x 5 days of Comp. 82/437 was found to eliminate almost 100% of adult worms and microfilariae of L. carinii in cotton rat. It also killed 100% and 97% of adult worms and microfilariae of Dipetalonema viteae and Brugia malayi in Mastomys natalensis respectively, at 150 and 200 mg/kg x 5 days orally. The compound also exhibited marked chemoprophylactic and in vitro activity against L. carinii.

摘要

已对2,2'-二羧甲氧基氨基-5,5'-二苯并咪唑基酮(II,中央药物研究所化合物82/437)针对啮齿动物体内卡里尼丝虫的微丝蚴和成虫杀灭效果进行了评估。发现给予82/437化合物3毫克/千克(腹腔注射)和50毫克/千克(口服),连续5天,可使棉鼠体内几乎100%的卡里尼丝虫成虫和微丝蚴被清除。在多乳鼠中,口服150毫克/千克和200毫克/千克,连续5天,该化合物还分别杀死了100%和97%的魏氏双瓣线虫和马来布鲁线虫的成虫和微丝蚴。该化合物对卡里尼丝虫还表现出显著的化学预防和体外活性。

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