Laboratory "Drug metabolism and drug toxicity", Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University-Sofia, Bulgaria; Department of Chemistry, Faculty of Pharmacy, Medical University-Sofia, Bulgaria.
Laboratory "Drug metabolism and drug toxicity", Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University-Sofia, Bulgaria; Department of Chemistry, Faculty of Pharmacy, Medical University-Sofia, Bulgaria.
Bioorg Med Chem. 2021 Jan 1;29:115888. doi: 10.1016/j.bmc.2020.115888. Epub 2020 Nov 27.
Selective monoamine oxidase type B (MAO-B) inhibitors are currently used as coadjuvants for treating early motor symptoms of Parkinson's disease. Aiming at the elucidation of MAO-B inhibitors with 1,3,4-oxadiazole scaffolds, we make a comprehensive update on the new and old chemical methods employed for the synthesis of the unsymmetrical oxadiazole derivatives that lead to high yield compounds. We summarize a state of the selective MAO-B inhibitors with oxadiazole scaffold, describing the results, structures, structure-activity relationships (SARs) and medicinal chemistry strategies over the years. The analysis of the recent papers would facilitate tracking the increasing number of oxadiazole derivatives as new chemical spaces with MAO-B inhibitory potential designed to ensure the safe use of the compounds and elimination of the unwanted drug-drug interactions.
选择性单胺氧化酶 B（MAO-B）抑制剂目前被用作治疗帕金森病早期运动症状的辅助药物。针对具有 1,3,4-恶二唑骨架的 MAO-B 抑制剂，我们全面更新了用于合成不对称恶二唑衍生物的新老化学方法，这些方法可以得到高产率的化合物。我们总结了具有恶二唑骨架的选择性 MAO-B 抑制剂的最新进展，描述了多年来的结果、结构、构效关系（SAR）和药物化学策略。对近期论文的分析将有助于跟踪越来越多的恶二唑衍生物作为具有 MAO-B 抑制潜力的新化学空间，以确保化合物的安全使用和消除不必要的药物相互作用。
