Department of Pharmaceutical Sciences, Northeastern Ohio Universities Colleges of Medicine and Pharmacy, 4209 State Route 44, Rootstown, OH 44272, USA.
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4798-803. doi: 10.1016/j.bmcl.2011.06.060. Epub 2011 Jun 21.
The neuroprotective activity of pioglitazone and rosiglitazone in the MPTP parkinsonian mouse prompted us to evaluate a set of thiazolidinedione (TZD) type compounds for monoamine oxidase A and B inhibition activity. These compounds were able to inhibit MAO-B over several log units of magnitude (82 nM to 600 μM). Initial structure-activity relationship studies identified key areas to modify the aromatic substituted TZD compounds. Primarily, substitutions on the aromatic group and the TZD nitrogen were key areas where activity was enhanced within this group of compounds.
吡格列酮和罗格列酮的神经保护活性在 MPTP 帕金森病小鼠中得到了验证，这促使我们评估了一组噻唑烷二酮（TZD）类化合物对单胺氧化酶 A 和 B 的抑制活性。这些化合物能够在几个数量级（82 nM 至 600 μM）的范围内抑制 MAO-B。初步的构效关系研究确定了需要修饰芳香取代 TZD 化合物的关键区域。主要是，芳香基团和 TZD 氮上的取代是该类化合物中活性增强的关键区域。
