In current study, we have designed and synthesized various indole functionalized piperazinyl derivatives. RP1 and RP9 emerged as most promising reversible MAO-A inhibitors with IC₅₀ values of 0.11±0.03 μM and 0.14±0.02 μM and displayed selectivity of 193- and 178-folds over MAO-B, respectively. RP1 showed good intracellular ROS inhibitory activity along with neuroprotective properties. During in vivo FST and TST studies, RP1 exhibited potential antidepressant-like behavior while compound RP9 showed antidepressant-like activity only in TST studies.

中文翻译：

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Indole-3-piperazinyl 衍生物作为潜在抗抑郁药的研究：设计、合成、体外、体内和计算机分析

在目前的研究中，我们设计并合成了各种吲哚官能化哌嗪基衍生物。RP1 和 RP9 成为最有希望的可逆 MAO-A 抑制剂，IC ₅₀值为 0.11±0.03 μM 和 0.14±0.02 μM，选择性分别是 MAO-B 的 193 倍和 178 倍。RP1 显示出良好的细胞内 ROS 抑制活性以及神经保护特性。在体内FST 和 TST 研究中，RP1 表现出潜在的抗抑郁样行为，而化合物 RP9 仅在 TST 研究中显示出抗抑郁样活性。