| Abstract
| - A series of pyrazinocarbazoles, analogues of short acting antidepressant pirlindole (2,3,3a,4,5,6-hexahydro-8-methyl-1H-pyrazino[3,2,1-j,k]carbazole hydrochloride), were tested as inhibitors of monoamine oxidaseA (MAO-A) and B (MAO-B). Rigid analogues exhibited potent and selective inhibition of MAO-A andhave size limits (X:Y:Z) of 13.0 × 7.0 × 4.4 Å. Besides MAO-A inhibition flexible analogues alsodemonstrated potent inhibition of MAO-B and in contrast to rigid analogues their inhibitory activity did notshow the dependence on these sizes. The qualitative information (steric and electrostatic coefficients) fromthe 3D-QSAR with CoMFA models for MAO-A and -B are different, and this information can be used todetermine the structural features influencing inhibitor selectivity.
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