Table 1. Inhibition percentage and IC50 values of the synthesized compounds, moclobemide, clorgyline, selegiline and safinamide against the MAO-A and MAO-B enzymes.
Compounds | MAO-A %inhibition |
MAO-A IC50 (μM) | MAO-B %inhibition |
|||||||||
10–3 M | 10–4 M | 10–5 M | 10–6 M | 10–7 M | 10–8 M | 10–9 M | 10–10 M | 10–11 M | 10–3 M | 10–4 M | ||
6a | 93.618 ± 1.974 | 89.506 ± 1.618 | 74.142 ± 1.296 | 61.895 ± 1.102 | 42.088 ± 0.955 | 30.268 ± 0.991 | 21.028 ± 0.882 | 14.201 ± 0.596 | 10.305 ± 0.411 | 0.336 ± 0.014 | 41.255 ± 0.985 | 22.352 ± 0.522 |
6b | 94.125 ± 2.884 | 91.548 ± 1.695 | 80.603 ± 1.541 | 72.675 ± 1.324 | 61.082 ± 0.979 | 34.748 ± 0.851 | 26.911 ± 0.805 | 20.074 ± 0.766 | 13.464 ± 0.510 | 0.060 ± 0.002 | 38.625 ± 0.856 | 25.741 ± 0.618 |
6c | 95.025 ± 1.902 | 91.102 ± 1.891 | 78.344 ± 1.456 | 62.311 ± 0.999 | 45.147 ± 0.933 | 25.133 ± 0.901 | 20.495 ± 0.896 | 12.036 ± 0.512 | 8.497 ± 0.385 | 0.241 ± 0.011 | 42.689 ± 0.966 | 26.788 ± 0.579 |
6d | 92.525 ± 2.011 | 89.142 ± 1.618 | 86.102 ± 1.903 | 46.039 ± 1.045 | 43.014 ± 0.919 | 23.882 ± 0.902 | 13.603 ± 0.588 | 10.801 ± 0.496 | 6.872 ± 0.297 | 1.073 ± 0.051 | 35.963 ± 0.715 | 28.455 ± 0.539 |
6e | 92.005 ± 1.809 | 86.418 ± 1.036 | 75.227 ± 1.419 | 56.496 ± 1.110 | 43.161 ± 0.982 | 32.693 ± 0.903 | 20.477 ± 0.872 | 13.529 ± 0.570 | 10.248 ± 0.423 | 0.502 ± 0.023 | 38.125 ± 0.795 | 29.221 ± 0.750 |
6f | 90.524 ± 2.015 | 82.308 ± 1.902 | 76.015 ± 1.408 | 47.321 ± 0.983 | 33.582 ± 0.991 | 29.963 ± 0.834 | 19.741 ± 0.716 | 11.088 ± 0.402 | 6.943 ± 0.285 | 1.175 ± 0.050 | 40.567 ± 0.825 | 34.322 ± 0.850 |
6g | 93.491 ± 1.988 | 84.276 ± 1.632 | 72.633 ± 1.408 | 43.189 ± 0.925 | 31.797 ± 0.903 | 25.495 ± 0.809 | 17.331 ± 0.700 | 12.645 ± 0.489 | 6.357 ± 0.296 | 1.786 ± 0.079 | 35.975 ± 0.723 | 24.162 ± 0.639 |
6h | 89.475 ± 1.465 | 41.378 ± 0.811 | — | — | — | — | — | — | — | — | 43.065 ± 0.899 | 20.711 ± 0.845 |
6i | 87.560 ± 1.288 | 42.659 ± 0.935 | — | — | — | — | — | — | — | — | 37.895 ± 0.735 | 26.505 ± 0.790 |
Moclobemide | 95.302 ± 2.658 | 83.145 ± 2.311 | 62.435 ± 1.894 | 35.756 ± 1.022 | 24.474 ± 0.997 | 19.635 ± 0.855 | 15.418 ± 0.725 | 12.849 ± 0.518 | 7.251 ± 0.289 | 4.664 ± 0.235 | — | — |
Clorgyline | 96.381 ± 2.055 | 92.148 ± 1.951 | 88.547 ± 1.816 | 79.115 ± 1.688 | 63.941 ± 1.021 | 35.259 ± 0.903 | 21.718 ± 0.750 | 16.995 ± 0.612 | 11.332 ± 0.484 | 0.048 ± 0.002 | — | — |
Selegiline | — | — | — | — | — | — | — | — | — | — | 98.258 ± 1.052 | 96.107 ± 1.165 |
Safinamide | — | — | — | — | — | — | — | — | — | — | 97.375 ± 2.048 | 94.455 ± 1.274 |