Bhat A R, Bhat G V, Shenoy G G
College of Pharmaceutical Sciences, Manipal, India.
J Pharm Pharmacol. 2001 Feb;53(2):267-72. doi: 10.1211/0022357011775307.
We have described the synthesis of new 1,2,4-triazoles and have evaluated their antimicrobial profile. Antitubercular activity was determined in triplicate using the Lowenstein-Jensen medium. A loopful of Mycobacterium tuberculosis suspension was inoculated on the surface of each Lowenstein-Jensen media containing the test compounds (100, 10 or 1 microg mL(-1)). To evaluate in-vitro antibacterial activity, compounds (50, 5 or 0.5 microg) were evaluated against B. subtilis, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Staphylococcus typhi by the disc diffusion method. To evaluate antifungal activity Sabourauds Dextrose agar medium was used. Some of the compounds (5, 0.5 or 0.05 microg mL(-1)) were screened for activity against Aspergillus niger 88 and Aspergillus niger 90 and others were screened for activity against T. rubrum TR1, T. rubrum R6, T. rubrum R7 and T. mentagrophyte M1, using the cup plate method. Our results show that the triazoles with a pyrazine moiety at position 3 were more active as antitubercular and antifungal agents compared with the triazoles which had a pyrazine moiety at position 4 of the molecule.
我们已经描述了新型1,2,4 - 三唑的合成,并评估了它们的抗菌谱。使用罗氏培养基一式三份测定抗结核活性。将一环结核分枝杆菌悬液接种在含有测试化合物(100、10或1微克/毫升)的每个罗氏培养基表面。为了评估体外抗菌活性,通过纸片扩散法评估化合物(50、5或0.5微克)对枯草芽孢杆菌、大肠杆菌、铜绿假单胞菌、金黄色葡萄球菌和伤寒沙门氏菌的抗菌活性。为了评估抗真菌活性,使用沙氏葡萄糖琼脂培养基。使用杯碟法,对一些化合物(5、0.5或0.05微克/毫升)进行针对黑曲霉88和黑曲霉90的活性筛选,对其他化合物进行针对红色毛癣菌TR1、红色毛癣菌R6、红色毛癣菌R7和须癣毛癣菌M1的活性筛选。我们的结果表明,与在分子4位具有吡嗪部分的三唑相比,在3位具有吡嗪部分的三唑作为抗结核和抗真菌剂更具活性。