Synthesis and Cholinesterase Inhibition Activity of New Pyrrolopyrimidine Derivatives

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.

Cite this article as:

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