Login

Journal Image
Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
Epub Full Text Article
DOI: 10.2174/1570180811666140704171902      Price:  $95









Synthesis and Cholinesterase Inhibition Activity of new Pyrrolopyrimidine Derivatives

img
Author(s): Rangaswamy Roopashree, Toreshettahally Ramesh Swaroop, Swamy Jagadish, Chakrabhavi Dhananjaya Mohan and Kanchugarakoppal Subbegowda Rangappa
Abstract:
Cholinesterase plays a vital role in the decline of cholinergic transmission and thus can contribute to 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 were 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
Affiliation:
Department of Studies in Chemistry University of Mysore Manasagangotri Mysore 570 006 India.