Abstract 1, 2, 3, 4-Tetrahydrobenzo [c]-1, 5-naphthyridine (5a) was prepared by a novel synthetic route involving the rearrangement of (±)-(Z)-1, 10a-dihydropyrrolo [1, 2-b] isoquinoline-3, 10 (2H, 5H)-dione oxime to afford 1, 4-dihydrobenzo [c]-1, 5-naphthyridin-2 (3H)-one, which was reduced to 5a. The cholinomimetic activity observed with 5a prompted the synthesis and biological evaluation of additional analogues.