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新型1,2,4-三嗪衍生物I 319的抗真菌特性

Antifungal properties of a novel 1,2,4-triazine derivative I 319.

作者信息

Wieczorek J, Mordarski M, Rykowski A, Nantka-Namirski P

出版信息

Arch Immunol Ther Exp (Warsz). 1980;28(5):727-33.

PMID:7212980
Abstract

The antifungal activity of the sodium salts, of 3-thiolo-5-phenyl-1,2,4-triazine (I 319) was determined in vitro and in vivo. The minimal inhibitory concentration (MIC) of I 319 for 33 pathogenic and saprophytic fungal strains ranged from 3.1 to 25 microgram/ml. In vivo, experiments were performed on a model of subacute candidiasis in Balb/c mice infected intraperitoneally with Candida albicans. The antifungal activity was estimated on the basis of the extension of the mice life span and on the number of living yeast cells present in the kidneys, liver and spleen of treated and control mice. A single i.p. dose of I 319 (25 mg/kg) prolonged the survival time of treated animals up to 200%. Five subsequent doses of the compound diminished the number of C. albicans cells in the tissues of these mice. The DL50 of I 319 for mice (i.p.) was about 250 mg/kg.

摘要

测定了3-硫醇基-5-苯基-1,2,4-三嗪(I 319)钠盐的体外和体内抗真菌活性。I 319对33种致病性和腐生性真菌菌株的最低抑菌浓度(MIC)范围为3.1至25微克/毫升。在体内,以腹腔注射白色念珠菌感染的Balb/c小鼠亚急性念珠菌病模型进行实验。根据小鼠寿命的延长以及治疗组和对照组小鼠肾脏、肝脏和脾脏中存活酵母细胞的数量来评估抗真菌活性。单次腹腔注射剂量的I 319(25毫克/千克)可使治疗动物的存活时间延长至200%。该化合物随后的五次给药减少了这些小鼠组织中白色念珠菌细胞的数量。I 319对小鼠的腹腔注射半数致死量(DL50)约为250毫克/千克。

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