This review presents a concise update on the inhibitors of the neuroenzyme, acetylcholinesterase (AChE; EC
18.104.22.168). AChE is a serine protease, which hydrolyses the neurotransmitter, acetylcholine into acetate and choline thereby
terminating neurotransmission. Molecular interactions (mode of binding to the target enzyme), clinical applications and
limitations have been summarized for each of the inhibitors discussed. Traditional inhibitors (e.g. physostigmine, tacrine,
donepezil, rivastigmine etc.) as well as novel inhibitors like various physostigmine-derivatives have been covered. This is
followed by a short glimpse on inhibitors derived from nature (e.g. Huperzine A and B, Galangin). Also, a discussion on
‘hybrid of pre-existing drugs’ has been incorporated. Furthermore, current status of therapeutic applications of AChEinhibitors
has also been summarized.