Background: Esterase is an enzyme that splits esters into an acid and alcohol. Varieties of
esterases are present in human body to control diverse set of cellular processes and execute their specific
functions. It can be seen that any increase in metabolites produced by these enzymes lead to severe
pathological conditions like Alzheimer disease, hypercholesterolemia etc.
Objective: Numerous esterase inhibitors have been developed and reported by the researchers around
the globe, but not systematically summarized yet. Therefore, this assemblage focuses on various reported
esterase inhibitors during recent past with detailed account of the design strategies employed for
the synthesis of novel drug entities. The article also highlights the structure activity relationship along
with mechanistic insights revealed during the biological evaluation of inhibitors as esterase inhibition.
The interactions with the amino acid residues responsible for esterase inhibitory potential of molecules
have also been discussed. This compilation will be of great interest for the researchers working in the
area of esterase inhibitors.
Conclusion: Rivastigmine derivatives (44-53), tacrine-piperazine hybrid (136), coumarin-benzofuran
derivative (169), coumarin-benzylpiperidine hybrid (181) and phenylcinnamide derivative (220) found
to be exerting cholinesterase inhibition with IC50 below the range of 1 nM. Whereas, flavone (258) has
displayed anticholesterol esterase potential below 1 nM. Benzil like derivative, (273) has also been designed
and reported to possess remarkable inhibitory potential (IC50 < 1 nM) against carboxylesterase.
These representative results place them in forefront as potential future drug candidates to further develop
potent and specific esterase inhibitors.