The purposes of this study were to synthesize new 3-benzazecine derivatives and investigate their chemical properties, as well as to preliminarily evaluate their in vitro biological properties as potential inhibitors of enzymes, which are drug targets related to neurological degenerative syndromes (e.g., Alzheimer and Parkinson diseases), namely, acetyl- and butyrylcholinesterases (AChE and BChE) and monoamine oxidases A and B (MAO-A and MAO-B). Here, MAOA is linked to Parkinson disease.