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.
Letters in Drug Design & Discovery
Title:Synthesis and Cholinesterase Inhibition Activity of New Pyrrolopyrimidine Derivatives
Volume: 11 Issue: 10
Author(s): Rangaswamy Roopashree, Toreshettahally Ramesh Swaroop, Swamy Jagadish, Chakrabhavi Dhananjaya Mohan and Kanchugarakoppal Subbegowda Rangappa
Affiliation:
Keywords: Acetylcholinesterase, alzheimer’s disease, butyrylcholinesterase, cholinergic transmission, inhibition, pyrrolopyrimidine.
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.
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Roopashree Rangaswamy, Ramesh Swaroop Toreshettahally, Jagadish Swamy, Dhananjaya Mohan Chakrabhavi and Subbegowda Rangappa Kanchugarakoppal, Synthesis and Cholinesterase Inhibition Activity of New Pyrrolopyrimidine Derivatives, Letters in Drug Design & Discovery 2014; 11 (10) . https://dx.doi.org/10.2174/1570180811666140704171902
DOI https://dx.doi.org/10.2174/1570180811666140704171902 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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