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Journal of enzyme inhibition and medicinal chemistry

Synthesis and initial results for MAO-B inhibition by new N-propargyl-3-pyrrol-1-ylindanamine derivatives, analogues of rasagiline.


PMID 12943198

Abstract

The syntthesis of new N-propargyl-3-pyrrol-1-ylindanamine derivatives, analogues of rasagiline, is described in ten steps starting from the corresponding arylaldehydes via the corresponding cis-3-pyrrol-1-ylindanamines. The cis-configuration of some intermediates has been established using X-ray analysis and NOE experiments. The new N-propargyl-3-pyrrol-1-ylindanamine derivatives were evaluated for their potential MAO-B inhibitor activity in an in vivo model of MPTP-induced Parkinsonism in mice with respect to the potent MAO-B inhibitor rasagiline.