抗真菌和抗分枝杆菌剂的研究。4-烷基硫代吡啶-2-碳硫酰胺的合成与活性。

Research on antifungal and antimycobacterial agents. Synthesis and activity of 4-alkylthiopyridine-2-carbothioamides.

作者信息

Klimesová V, Svoboda M, Waisser K, Machácek M, Buchta V, Odlerová Z

机构信息

Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Hradec Králové, Czech Republic.

出版信息

Arch Pharm (Weinheim). 1996 Oct;329(10):438-42. doi: 10.1002/ardp.19963291003.

DOI:10.1002/ardp.19963291003

PMID:8933745

Abstract

A series of 4-alkylthiopyridine-2-carbothioamides have been prepared and evaluated in vitro for antimicrobial activity. Chemical structures have been demonstrated by IR and 1H NMR data and by elemental analysis. The antimycobacterial activity of these compounds against Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium avium, and Mycobacterium fortuitum, and the antifungal activity against Candida albicans, Candida tropicalis, Candida krusei, Candida glabrata, Trichosporon beigelii, Trichophyton mentagrophytes, Aspergillus fumigatus, and Absidia corymbifera were determined by the MIC values. Compounds 3 exhibit good antimycobacterial activity compared to isoniazide. A moderate antifungal activity was observed against T. mentagrophytes. Activity is influenced by hydrophobicity of the alkyl group.

摘要

已制备了一系列4-烷基硫代吡啶-2-碳硫酰胺，并在体外评估了其抗菌活性。通过红外光谱、¹H核磁共振数据和元素分析确定了化学结构。通过最低抑菌浓度（MIC）值测定了这些化合物对结核分枝杆菌、堪萨斯分枝杆菌、鸟分枝杆菌和偶然分枝杆菌的抗分枝杆菌活性，以及对白色念珠菌、热带念珠菌、克柔念珠菌、光滑念珠菌、白吉利毛孢子菌、须癣毛癣菌、烟曲霉和伞枝犁头霉的抗真菌活性。与异烟肼相比，化合物3表现出良好的抗分枝杆菌活性。观察到对须癣毛癣菌有中等程度的抗真菌活性。活性受烷基疏水性的影响。