Department of Chemistry, Guru Nanak Dev University, Amritsar-143005, Punjab, India.
Dalton Trans. 2012 May 21;41(19):5778-81. doi: 10.1039/c2dt30514c. Epub 2012 Apr 3.
Twenty different triazoles were prepared to probe the anti-tubercular structure-activity relationships (SAR) within the β-lactam-ferrocene-triazole conjugate family. The compounds have been synthesized by copper-catalyzed "click chemistry". In vitro anti-tubercular activity was determined for each compound but the synthesized hybrids failed to inhibit Mycobacterium tuberculosis growth even at high doses. The manuscript assumes significance as this is the first report on the inclusion of ferrocene nucleus in the well established β-lactam family via triazole linkers with reputed physicochemical profiles.
为了探索β-内酰胺-二茂铁-三唑偶联物家族中的抗结核结构-活性关系(SAR),我们制备了二十种不同的三唑。这些化合物是通过铜催化的“点击化学”合成的。我们已经测定了每种化合物的体外抗结核活性,但这些合成的杂化物即使在高剂量下也未能抑制结核分枝杆菌的生长。这篇论文具有重要意义,因为这是首次通过具有良好理化特性的三唑连接体将二茂铁核纳入成熟的β-内酰胺家族的报道。