Shiradkar Mahendra, Suresh Kumar Gorentla Venkata, Dasari Varaprasad, Tatikonda Suresh, Akula Kalyan Chakravarthy, Shah Rachit
Dr. Reddys Laboratories, Research and Development, 7-1-27, Ameerpet, Hyderabad-500016, Andhra Pradesh, India.
Eur J Med Chem. 2007 Jun;42(6):807-16. doi: 10.1016/j.ejmech.2006.12.001. Epub 2006 Dec 15.
In last few decades, though significant progress has been made in the treatment and control strategies of tubercular infections by introducing new diagnostic and monitoring tools and combination therapy, it still continues to be a severe problem. Thus with the aim of developing novel molecules with improved potency for treating Mycobacterium tuberculosis H37Rv strain infections and with decreased probability of developing drug resistance, herein we report the synthesis of thiazolyl triazole derivatives, starting from ethyl acetoacetate, by microwave organic reaction enhancement method (MORE) and results of investigations of their antimycobacterial and antimicrobial activities. Many compounds have shown promising activity while others were inactive.
在过去几十年里，尽管通过引入新的诊断和监测工具以及联合疗法，结核感染的治疗和控制策略取得了显著进展，但它仍然是一个严重的问题。因此，为了开发具有更高效力以治疗结核分枝杆菌H37Rv菌株感染且产生耐药性可能性降低的新型分子，在此我们报告了从乙酰乙酸乙酯出发，通过微波有机反应增强法（MORE）合成噻唑基三唑衍生物及其抗分枝杆菌和抗菌活性的研究结果。许多化合物显示出有前景的活性，而其他一些则无活性。
