Inhibition of monoamine oxidases by benzimidazole chalcone derivatives

Applied Biological Chemistry

Table 1 Inhibitions of MAO-A and MAO-B by benzimidazole chalcone derivatives^a

Compound	Residual activity at 10 μM (%)		IC₅₀ (μM)		SI
Compound	MAO-A	MAO-B	MAO-A	MAO-B	SI
BCH1	98.73 ± 10.74	99.95 ± 7.69	> 40	> 40	–
BCH2	76.00 ± 1.89	4.05 ± 1.91	35.29 ± 4.55	0.80 ± 0.0094	44.11
BCH3	37.50 ± 4.65	35.05 ± 7.27	5.59 ± 1.12	4.83 ± 0.76	1.16
BCH4	83.33 ± 0.94	16.48 ± 2.41	27.17 ± 0.14	1.11 ± 0.17	24.48
BCH5	43.38 ± 6.08	41.3 ± 7.69	8.39 ± 0.70	6.87 ± 1.79	1.22
BCH6	26.63 ± 0.77	23.36 ± 0.58	1.63 ± 0.10	2.04 ± 0.13	0.80
BCH7	83.70 ± 1.54	50.54 ± 1.52	> 40	10.94 ± 0.89	3.66
BCH8	82.28 ± 1.79	47.52 ± 0.98	> 40	8.32 ± 1.53	4.81
BCH9	78.48 ± 3.59	51.76 ± 3.33	> 40	10.02 ± 0.30	3.99
BCH10	87.5 ± 8.84	48.78 ± 6.90	> 40	11.09 ± 0.07	3.61
Toloxatone	–	–	1.646 ± 0.094	–
Lazabemide	–	–	–	0.073 ± 0.0013
Clorgyline	–	–	0.0079 ± 0.00094	–
Pargyline	–	–	–	0.11 ± 0.011

^aResults are presented as the means ± standard error of duplicate or triplicate experiments
^bSelectivity index (SI) are calculated for MAO-B using IC₅₀ values, i.e., IC₅₀ of MAO-A/ IC₅₀ of MAO-B