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Publication Type : Journal Article
Publisher : Medchemcomm
Source : Medchemcomm, Volume 9, Issue 11, p.1871-1881 (2018)
Campus : Kochi
School : School of Pharmacy
Department : Pharmaceutical Chemistry & Analysis
Year : 2018
Abstract : A series of 13 phenyl substituted thiosemicarbazones () were synthesized and evaluated for their inhibitory potential towards human recombinant monoamine oxidase A and B (MAO-A and MAO-B, respectively) and acetylcholinesterase. The solid state structure of was ascertained by the single X-ray diffraction technique. Compounds and were potent for MAO-A (IC 1.82 ± 0.14) and MAO-B (IC 0.27 ± 0.015 μM), respectively. Furthermore, showed a high selectivity index (SI > 37.0) for MAO-B. The effects of fluorine orientation revealed that (-fluorine) showed 28.2 times higher inhibitory activity than (-fluorine) against MAO-B. Furthermore, inhibitions by and against MAO-A and MAO-B, respectively, were recovered to near reference levels in reversibility experiments. Both and showed competitive inhibition modes, with values of 0.97 ± 0.042 and 0.12 ± 0.006 μM, respectively. These results indicate that and are selective, reversible and competitive inhibitors of MAO-A and MAO-B, respectively. Compounds , and showed moderate inhibition against acetylcholinesterase with IC values of 35.35 ± 0.47, 15.61 ± 0.057 and 26.61 ± 0.338 μM, respectively. Blood-brain barrier (BBB) permeation was studied using the parallel artificial membrane permeation assay (PAMPA) method. Molecular docking studies were carried out using AutoDock 4.2.
Cite this Research Publication : Bijo Mathew, Baek, S. Cheol, Parambi, D. Grace Thom, Lee, J. Pil, Joy, M., Rilda, P. R. Annie, Randev, R. V., Nithyamol, P., Vijayan, V., Inasu, S. T., Mathew, G. Elizabeth, Lohidakshan, K. K., Krishnan, G. Kumar, and Kim, H., “Selected aryl thiosemicarbazones as a new class of multi-targeted monoamine oxidase inhibitors.”, Medchemcomm, vol. 9, no. 11, pp. 1871-1881, 2018.