ASSESSMENT OF ANTIMYCOBACTERIAL ACTIVITY OF PROPYLTHIADIAZOLOQUINAZOLINE DERIVATIVES AGAINST MYCOBACTERIUM INTRACELLULARE

O. G. Sechko, N. Gurina, V. M. Tsarenkov, I. Slabko, F. Macaev, A. Uncu, V. Valica
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Abstract

The compounds studied are propylthiadiazoloquinazoline derivatives, tryptanthrin analogs. Tryptantrin and its derivatives were found to have different antimycobacterial activity in vitro and in vivo. This series of experiments is devoted to the study of antimycobacterial activity of three propylthiadiazoloquinazoline derivatives obtained in the laboratory of organic synthesis and Biopharmaceutics of the Institute of Chemistry of the Academy of Sciences in Moldova using a non-tuberculous strain of Mycobacterium intracellulare, which is a part of the Mycobacterium avium complex (MAC). Species of the MAC are one of the main pathogen types causing mycobacteriosis. In this regard, propylthiadiazoloquinazoline derivatives are of interest for a comprehensive study as a potential antimycobacterial drug. To study antimycobacterial activity the method of dilutions in a dense nutrient medium of Middlebrook 7H9 broth with glycerol in Petri dishes was used. To assess antimycobacterial activity visual assessment of M. intracellulare growth in a solid nutrient medium was used. It is shown that the compounds studied inhibit M. Intracellulare growth. The most active compound was compound № 1 - 2-mercapto-5H-[1,3,4]-thiadiazolo-[2,3-b]-quinazoline-5-one.
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丙基噻二唑喹啉衍生物对细胞内分枝杆菌的抑菌活性评价
所研究的化合物是丙基噻二唑喹啉衍生物、色氨酸类似物。在体外和体内实验中发现,色坦素及其衍生物具有不同的抑菌活性。这一系列实验致力于研究摩尔多瓦科学院化学研究所有机合成和生物制药实验室获得的三种丙基噻二唑啉衍生物的抗细菌活性,使用的是非结核分枝杆菌胞内菌株,该菌株是鸟分枝杆菌复合体(MAC)的一部分。MAC是引起分枝杆菌病的主要病原体类型之一。在这方面,丙基噻二唑喹啉衍生物作为一种潜在的抗细菌药物值得全面研究。为了研究米德尔布鲁克7H9肉汤的抑菌活性,采用了在培养皿中用甘油稀释浓营养培养基的方法。为了评估抗菌活性,采用了固体营养培养基中芽孢杆菌胞内生长的目测法。结果表明,所研究的化合物可抑制胞内分枝杆菌的生长。活性最高的化合物为1 - 2-巯基- 5h -[1,3,4]-噻二唑-[2,3-b]-喹唑啉-5- 1化合物。
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