Herein, twenty‐one dantrolene‐like hydrazide and hydrazone analogues were synthesized with the aim of exploring structure‐activity relationships (SARs) for the inhibition of human monoamine oxidases (MAOs) and acetylcholinesterase (AChE), two well‐established target enzymes for anti‐AD drugs. The gene discussed is ACHE; the disease is Alzheimer disease.