超氧化物歧化酶模拟物：MnTBAP类似物的合成及其构效关系研究
Superoxide dismutase mimetics: synthesis and structure-activity relationship study of MnTBAP analogues.
作者信息
Gauuan Polivina Jolicia F, Trova Michael P, Gregor-Boros Livia, Bocckino Stephen B, Crapo James D, Day Brian J
机构信息
Albany Molecular Research, Inc., 21 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA.
出版信息
Bioorg Med Chem. 2002 Sep;10(9):3013-21. doi: 10.1016/s0968-0896(02)00153-0.
Carboxylic ester and amide-substituted analogues of [5,10,15,20-tetrakis(4-carboxyphenyl)-porphyrinato]manganese(III) chloride (MnTBAP) were synthesized and assayed as potential superoxide dismutase (SOD) mimetics. The tetraester analogues 4a and 4b were found to have comparable SOD activity to the known SOD mimetic MnTBAP, while amides 4c-4e exhibited reduced SOD activity. In the substituted methyl benzoate/acid and disubstituted porphyrin series, analogues 12c, 12f, and 12m were found to have comparable to improved SOD activity relative to MnTBAP and analogues 12j, 13a, and 13d exhibited improved activity in both the SOD and thiobarbituric acid reactive species (TBARS) assays relative to MnTBAP.
合成了[5,10,15,20-四（4-羧基苯基）-卟啉锰（III）]氯化物（MnTBAP）的羧酸酯和酰胺取代类似物，并作为潜在的超氧化物歧化酶（SOD）模拟物进行了测定。发现四酯类似物4a和4b具有与已知的SOD模拟物MnTBAP相当的SOD活性，而酰胺4c-4e的SOD活性降低。在取代的苯甲酸甲酯/酸和二取代卟啉系列中，发现类似物12c、12f和12m相对于MnTBAP具有相当或更高的SOD活性，并且类似物12j、13a和13d相对于MnTBAP在SOD和硫代巴比妥酸反应性物质（TBARS）测定中均表现出更高的活性。
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