2018
DOI: 10.3390/molecules23010113
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Design, Synthesis and Biological Evaluation of Novel N-Pyridyl-Hydrazone Derivatives as Potential Monoamine Oxidase (MAO) Inhibitors

Abstract: A new series of N-pyridyl-hydrazone derivatives was synthesized by using a simple and efficient method. The final compounds obtained were screened for their inhibitory potency against monoamine oxidase (MAO) A and B. The newly synthesized compounds 2a–2n specifically inhibited monoamine oxidases, displaying notably low IC50 values. Compounds 2i and 2j, with a CF3 and OH group on the 4-position of the phenyl ring, respectively, showed considerable MAO-A and MAO-B inhibitory activities. Compounds 2k, 2l and 2n, … Show more

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Cited by 22 publications
(6 citation statements)
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“…In contrast, compounds 2d and 2j , with para -F and para -Br groups on the benzyl ring, respectively, selectively inhibited MAO-A, with IC 50 values of 1.38 and 2.48 µM, respectively. Selective MAO-A inhibitors are suitable for the treatment of anxiety and depression [ 30 ], whereas MAO-B inhibitors are suitable for the treatment of Parkinson’s disease (PD) and AD [ 31 ]. Many selective inhibitors for MAO-A and MAO-B have been reported, and some are now used to treat neurological disorders in the clinic [ 32 , 33 ].…”
Section: Resultsmentioning
confidence: 99%
“…In contrast, compounds 2d and 2j , with para -F and para -Br groups on the benzyl ring, respectively, selectively inhibited MAO-A, with IC 50 values of 1.38 and 2.48 µM, respectively. Selective MAO-A inhibitors are suitable for the treatment of anxiety and depression [ 30 ], whereas MAO-B inhibitors are suitable for the treatment of Parkinson’s disease (PD) and AD [ 31 ]. Many selective inhibitors for MAO-A and MAO-B have been reported, and some are now used to treat neurological disorders in the clinic [ 32 , 33 ].…”
Section: Resultsmentioning
confidence: 99%
“…As toxicity is one of the filtering stage for drug candidate, in preclinical phases, cytotoxicity assays performed on new drug candidate to select more safe and appropriate drugs. [ 55 ] Based on ISO recommendation (10993‐5, 2009), NIH/3T3 is a good choice for evaluation of cytotoxic potential of candidate drugs. [ 56 ] In addition to NIH/3T3 (murine embryonic fibroblast) as a normal cell line, we also examined the effects of the synthesized substances on breast cancer cells (MCF‐7).…”
Section: Methodsmentioning
confidence: 99%
“…The SAR revealed that the m ‐Nitrophenyl at C4 position as in compound 34 , on the hydrothiazole nucleus is important for selectivity against human MAO‐B enzyme (Figure 4). Synthesis was carried out by treatment of alkyl‐aryl ketones with thiosemicarbazides with acetic acid and then 2‐bromo‐3’‐nitroacetophenone by Hantzsch reaction to prepare final derivatives [135] …”
Section: Synthetic Approaches and Design Aspects Of Various Classes Omentioning
confidence: 99%