作为抗结核药物的羧脒腙类似物的金属配合物。1. 合成、X射线晶体结构、光谱性质及对结核分枝杆菌H(37)Rv的抗分枝杆菌活性。
Metal complexes of carboxamidrazone analogs as antitubercular agents. 1. Synthesis, X-ray crystal-structures, spectroscopic properties and antimycobacterial activity against Mycobacterium tuberculosis H(37)Rv.
作者信息
Sandbhor Uday, Padhye Subhash, Billington David, Rathbone Daniel, Franzblau Scott, Anson Christopher E, Powell Annie K
机构信息
Department of Chemistry, University of Pune, Pune 411 007, India.
出版信息
J Inorg Biochem. 2002 Jun 7;90(3-4):127-36. doi: 10.1016/s0162-0134(02)00406-3.
N(1)-Benzylidene-pyridine carboxamidrazones and their metal conjugates have emerged as a new class of potential antimycobacterial agents. Nine such carboxamidrazone analogs (L(1)-L(9)) along with their Cu(II) (MC(1)-MC(9)) and Fe(III) (MC(10)-MC(18)) complexes were synthesized. Single crystal X-ray structures of copper complexes MC(1) and MC(5) were determined which suggest slightly distorted square planer geometries for copper complexes and octahedral geometries for ferric compounds. All compounds were evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H(37)Rv. The results show 32-64-fold enhancement in antitubercular activity upon copper complexation.
N(1)-亚苄基吡啶甲脒及其金属共轭物已成为一类新型潜在抗分枝杆菌药物。合成了九种此类甲脒类似物（L(1)-L(9)）及其铜（II）配合物（MC(1)-MC(9)）和铁（III）配合物（MC(10)-MC(18)）。测定了铜配合物MC(1)和MC(5)的单晶X射线结构，结果表明铜配合物的几何形状为稍有扭曲的平面正方形，铁化合物的几何形状为八面体。评估了所有化合物对结核分枝杆菌H(37)Rv的体外抗分枝杆菌活性。结果表明，与铜络合后抗结核活性提高了32至64倍。
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