The sulfur analogs of harmaline, 7‐methoxy‐3,4‐dihydro‐1‐methyl[1]benzothieno[2,3‐c]‐pyridine (Ib), harmine, 7‐methoxy‐1‐methyl[1]benzothieno[2,3‐c]pyridine (IIb), and corresponding 6‐methoxy isomers (Ic and IIc) have been synthesized for pharmacological evaluation as monoamine oxidase inhibitors.