Synthesis and cholinesterase inhibition activity of new pyrrolopyrimidine derivatives

Roopashree, R. and Swaroop, T. R. and Jagadish, S. and Mohan, C. D. and Rangappa, K. S. (2014) Synthesis and cholinesterase inhibition activity of new pyrrolopyrimidine derivatives. Letters in Drug Design and Discovery, 11 (10). pp. 1143-1148.

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Official URL: http://doi.org/10.2174/1570180811666140704171902

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-dpyrimidin-6-yl)benzoate was the most potent molecule identified with the IC50 values of 18 μM and 17 uM on AChe and BuChe respectively.

Item Type: Article
Uncontrolled Keywords: Article, drug potency, drug synthesis, IC50, in vitro study, proton nuclear magnetic resonance, unclassified drug, priority journal, acetylcholinesterase, cholinesterase, cholinesterase inhibition, Alzheimer disease, blood sampling, 3 d]pyrimidin 6 yl]benzoate, 3 d]pyrimidin 6yl]benzoate, cholinergic transmission, ethyl 4 4 (3 chlorophenylamino) 7h pyrrolo2, ethyl 4 4 (3 fluorophenylamino) 7h pyrrolo2, ethyl 4 4 (3 methoxyphenylamino) 7h pyrrolo2, ethyl 4 4 (4 bromophenylamino) 7h pyrrolo2, ethyl 4 4 (4 fluorophenylamino) 7h pyrrolo2, ethyl 4 4 (4 methoxyphenylamino) 7h pyrrolo2, ethyl 4 4 (p tolylamino) 7h pyrrolo2, ethyl 4 4 (phenylamino) 7h pyrrolo2, optical density, pyrrolopyrimidine derivative
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: Arshiya Kousar Library Assistant
Date Deposited: 21 Aug 2019 07:13
Last Modified: 21 Aug 2019 07:13
URI: http://eprints.uni-mysore.ac.in/id/eprint/4378

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