Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Matunga, Mumbai, India.
Bioorg Med Chem Lett. 2012 Mar 15;22(6):2343-6. doi: 10.1016/j.bmcl.2012.01.067. Epub 2012 Feb 4.
Tuberculosis constitutes today a serious threat to human health worldwide, aggravated by the increasing number of identified multi-drug resistant strains of Mycobacterium tuberculosis (Mtb), its causative agent, as well as by the lack of development of novel mycobactericidal compounds for the last few decades. A novel series of benzofuran-3-carbohydrazide and its analogs was synthesized and characterized spectroscopically. All the compounds were characterized and screened for in vitro anti-tuberculosis (anti-TB) activity against Mycobacterium tuberculosis H37Rv strains by using resazurin assay utilizing microtiter-plate method (REMA). These compounds also showed good antifungal activity against Candida albicans. Thus, the high level of activity shown by the compounds (8a, 8k) suggests that these compounds could serve as leads for development of novel synthetic compounds with enhanced anti-TB and antifungal activity.
结核病目前是全球范围内对人类健康的严重威胁，其原因包括结核分枝杆菌（Mtb）的耐药菌株数量不断增加，以及过去几十年中新型分枝杆菌杀菌化合物的研发缺乏。我们合成并通过光谱学进行了一系列新的苯并呋喃-3-甲酰肼及其类似物的表征。所有化合物都通过微量板法（REMA）利用 Resazurin 测定法进行了结核分枝杆菌 H37Rv 菌株的体外抗结核（抗-TB）活性的特征和筛选。这些化合物对白色念珠菌也表现出良好的抗真菌活性。因此，这些化合物（8a、8k）表现出的高活性表明，这些化合物可以作为开发具有增强抗结核和抗真菌活性的新型合成化合物的先导。
