Synthesis and Cholinesterase Inhibition Activity of New Pyrrolopyrimidine Derivatives

Author(s): Rangaswamy Roopashree, Toreshettahally Ramesh Swaroop, Swamy Jagadish, Chakrabhavi Dhananjaya Mohan, Kanchugarakoppal Subbegowda Rangappa

Journal Name: Letters in Drug Design & Discovery

Volume 11 , Issue 10 , 2014

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Graphical Abstract:


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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Article Details

Year: 2014
Published on: 04 July, 2014
Page: [1143 - 1148]
Pages: 6
DOI: 10.2174/1570180811666140704171902
Price: $65

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