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Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
VOLUME: 11
ISSUE: 10
DOI: 10.2174/1570180811666140704171902      Price:  $58









Synthesis and Cholinesterase Inhibition Activity of New Pyrrolopyrimidine Derivatives

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Author(s): Rangaswamy Roopashree, Toreshettahally Ramesh Swaroop, Swamy Jagadish, Chakrabhavi Dhananjaya Mohan and Kanchugarakoppal Subbegowda Rangappa
Pages 1143-1148 (6)
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.
Graphical Abstract:
Keywords:
Acetylcholinesterase, alzheimer’s disease, butyrylcholinesterase, cholinergic transmission, inhibition, pyrrolopyrimidine.
Affiliation:
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India.