Mohite P B, Bhaskar V H
Department of Pharmaceutical chemistry,MES College of Pharmacy,Sonai, Ahmednagar, Maharashtra,India. ; Research Scholar,Department of Pharmacy,Vinayaka Missions University,Salem,Tamilnadu,India.
Adv Pharm Bull. 2012;2(1):31-6. doi: 10.5681/apb.2012.005. Epub 2012 Feb 15.
We report here the antimycobacterial activity of some already synthesized tetrazole derivatives containing tetrazole against Mycobacterium tuberculosis strain H37Rv.
In vitro evaluation of the antitubercular activity was carried out within the Tuberculosis Antimicrobial Acquisition & Coordinating Facility (TAACF) screening program for the discovery of novel drugs for the treatment of tuberculosis. Under the direction of the US National Institute of Allergy and Infectious Diseases (NIAID), Southern Research Institute that coordinates the overall program. The method of TAACF was followed for evaluation of activity.
This new structural class of compounds showed high activity against the bacilli. The activity depends on the substituent's present in azatidinone core. Compounds having a 4-MeOC6H4 4-N(CH3)2C6H4 group as the substituent on β-lactam ring were active. The highest activity was registered for compounds having 4-MeOC6H4 as substituent.
The new compounds showed high potency and promising antitubercular activity and should be regarded as new hits for further development as a novel class of Antimycobacterium tuberculosis agents.
我们在此报告一些已合成的含四氮唑的四氮唑衍生物对结核分枝杆菌H37Rv菌株的抗分枝杆菌活性。
在结核病抗菌药物采购与协调设施（TAACF）筛选项目中进行了抗结核活性的体外评估，该项目旨在发现治疗结核病的新药。在美国国家过敏和传染病研究所（NIAID）的指导下，由南方研究所协调整个项目。按照TAACF的方法评估活性。
这类新的化合物对杆菌显示出高活性。活性取决于氮杂环丁烷酮核心中存在的取代基。在β-内酰胺环上具有4-MeOC6H4 4-N(CH3)2C6H4基团作为取代基的化合物具有活性。以4-MeOC6H4作为取代基的化合物活性最高。
这些新化合物显示出高效力和有前景的抗结核活性，应被视为作为新型抗结核分枝杆菌药物进一步开发的新苗头。
