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某些4-烷基氨基-2/3-甲氧基-4-氨基二苯砜的抗疟活性。

Antimalarial activity of some 4-alkylamino 2/3 methoxy-4-aminodiphenyl sulphones.

作者信息

Chandra S, Raina R, Sen A B, Saxena M, Saxena A K

机构信息

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

出版信息

Indian J Malariol. 1990 Sep;27(3):163-6.

PMID:2292320
Abstract

From a series of thirty six 2,3, N-substituted 4,4'-diaminodiphenyl sulphones studied for their suppressive activity in mice against blood induced erythrocytic stage of Plasmodium berghei infection, six sulphones (1-6) showed 100% suppressive and curative activity at an intraperitoneal dose of 1 mg/kg x 4 days. These sulphones have been studied for their suppressive activity in still lower doses ranging from 1.0-0.25 mg/kg i.p. x 4 days and for their curative activity at 1 mg/kg i.p. x 4 days in comparison to DDS as standard drug. The maximum tolerated dose of these compounds and DDS has also been determined. These sulphones have better therapeutic efficacy for their suppressive and curative action than DDS.

摘要

在对36种2,3, N-取代的4,4'-二氨基二苯砜进行的一系列研究中,考察了它们对感染伯氏疟原虫的小鼠血液诱导红细胞期的抑制活性。其中6种砜类化合物(1-6)在腹腔注射剂量为1mg/kg×4天的情况下,显示出100%的抑制和治愈活性。已研究了这些砜类化合物在1.0-0.25mg/kg腹腔注射×4天的更低剂量下的抑制活性,以及与作为标准药物的氨苯砜相比,在1mg/kg腹腔注射×4天的治愈活性。还测定了这些化合物和氨苯砜的最大耐受剂量。与氨苯砜相比,这些砜类化合物在抑制和治愈作用方面具有更好的治疗效果。

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