Synthesis and Cholinesterase Inhibition Activity of New Pyrrolopyrimidine Derivatives
Rangaswamy Roopashree, Toreshettahally Ramesh Swaroop, Swamy Jagadish, Chakrabhavi Dhananjaya Mohan and Kanchugarakoppal Subbegowda Rangappa
Affiliation: Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India.
Cholinesterase plays a vital role in the decline of cholinergic transmission and thus can contribute to the development
of Alzheimer’s disease (AD). Thus, compounds that can inhibit acetylcholinesterase (AChe) and butyrylcholinesterase
(BuChe) are the potential drugs for the treatment of AD. A series of novel pyrrolopyrimidine derivatives was
synthesized and evaluated for their inhibitory activity against cholinesterase by Ellman method. Among the ten newly
synthesized compounds, 4-(4-((4-(difluoromethoxy)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)benzoate was the
most potent molecule identified with the IC50 values of 18 µM and 17 µM on AChe and BuChe respectively.
Keywords: Acetylcholinesterase, alzheimer’s disease, butyrylcholinesterase, cholinergic transmission, inhibition, pyrrolopyrimidine.
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