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Triphenylpyrazoline ketone chlorophenols as potential candidate compounds against Parkinson’s disease: design, synthesis, and biological evaluation by Ning Ning Cheng; Le Hua Zhang; Rui Ge; Xiu E. Feng; Qing Shan Li is a Chemistry article available to read on EtoBox.

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Parkinson's disease (PD) is a progressively neurodegenerative disease following dopamine neuron loss and motor dysfunction. Selective monoamine oxidase B (MAO-B) inhibitors are regarded as the potential candidates for the treatment of PD. 2-Pyrazoline structure, an important pharmacodynamic parent nucleus of MAO inhibitors, was introduced into the lead compound 2,3-dibromo-4,5-dihydroxylbenzophenone (LM48), thirty-two triphenylpyrazoline ketone chlorophenols were therefore synthesized, and their protective activities against 6-hydroxydopamine damaged SH-SY5Y cells were further evaluated. Seven chlorophenols 9d, 11d, 28d, 29d, 30d, 31d, and 32d exhibited the significant protective activity with the EC 50 values in the range of 0.3-1.2 μM, superior to LM48 (EC 50 > 20 μM) and Rasagiline (EC 50 = 1.1 ± 0.6 μM). Moreover, they could obviously reduce ROS level. Their MAO-A and MAO-B inhibitory activities in vitro were further compared. MAO-A inhibitory activity was not found at 50 μM, but sixteen compounds were discovered showing selective MAO-B inhibitory activity. Of which, compound 6d presented the optimal activity (IC 50 = 12.2 ± 2.3 μM). Compared with Rasagiline (an irreversible MA

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Author

Ning Ning Cheng; Le Hua Zhang; Rui Ge; Xiu E. Feng; Qing Shan Li

Publisher

Springer Science and Business Media LLC

Published

2022

Language

EN

Field

Chemistry (Physical Sciences)