Synthesis, characterization and pharmacological evaluation of pyrimidine analogues for the management of Alzheimer’s disease

Abstract

Event Abstract Back to Event Synthesis, characterization and pharmacological evaluation of pyrimidine analogues for the management of Alzheimer’s disease Rakesh Yadav1*, Monika Maan1 and Divya Yadav1 1 Banasthali University, Pharmaceutical Chemistry, India Alzheimer’s disease (AD) is a highly complex neurodegenerative disorder, which is characterized by the loss of memory and manifests in the cholinergic branch of central nervous system. Cholinesterase inhibitors have been found to be efficacious in reducing the symptoms of early medium stage of AD. There are number of drugs, which have been reported such as donepezil, galantamine, tacrine for the treatment of Alzheimer's. The pyrimidine scaffold is an important pharmacological structural component in well-known anti-AD drugs. In the present study, we have designed, synthesized and evaluated a series of 2, 4-disubstituted pyrimidine derivatives (RY-114 to RY-123) for the treatment of neurodegenerative diseases. The synthesis of a key intermediate i.e. 4-(substituted aniline)-2-chloropyrimidine was performed using 2, 4-dichloropyrimidine (1) as a starting material. The condensation of 1 with various substituted aniline in the presence of DIPEA and ethanol gave the desired key intermediate. The titled compounds were synthesized by condensation of the key intermediate with various primary or secondary substituted amines using direct fusion method in microwave or reflux in the presence of DIPEA and n-butanol. The structures of newly synthesized compounds were characterized using various spectral techniques viz. FT-IR, NMR, elemental analysis etc. The biological evaluation (in vivo or in vitro) of the synthesized derivatives RY-114 to RY-123 showed gradient effect with respect to the standard drug (Donezepil). The outcome of the work may lead to be selective and medicinally active chemical entities for the management of Alzheimer’s disease. Keywords: Galantamine, Tacrine, Alzheimer’s disease, donepezil, Neurodegenerative disorders Conference: 14th Meeting of the Asian-Pacific Society for Neurochemistry, Kuala Lumpur, Malaysia, 27 Aug - 30 Aug, 2016. Presentation Type: YIC04: Young Investigator Colloquium 4 Topic: 14th Meeting of the Asian-Pacific Society for Neurochemistry Citation: Yadav R, Maan M and Yadav D (2016). Synthesis, characterization and pharmacological evaluation of pyrimidine analogues for the management of Alzheimer’s disease. Conference Abstract: 14th Meeting of the Asian-Pacific Society for Neurochemistry. doi: 10.3389/conf.fncel.2016.36.00065 Copyright: The abstracts in this collection have not been subject to any Frontiers peer review or checks, and are not endorsed by Frontiers. They are made available through the Frontiers publishing platform as a service to conference organizers and presenters. The copyright in the individual abstracts is owned by the author of each abstract or his/her employer unless otherwise stated. Each abstract, as well as the collection of abstracts, are published under a Creative Commons CC-BY 4.0 (attribution) licence (https://creativecommons.org/licenses/by/4.0/) and may thus be reproduced, translated, adapted and be the subject of derivative works provided the authors and Frontiers are attributed. For Frontiers’ terms and conditions please see https://www.frontiersin.org/legal/terms-and-conditions. Received: 04 Aug 2016; Published Online: 11 Aug 2016. * Correspondence: Dr. Rakesh Yadav, Banasthali University, Pharmaceutical Chemistry, Banasthali, Rajasthan, India, rakesh_pu@yahoo.co.in Login Required This action requires you to be registered with Frontiers and logged in. To register or login click here. Abstract Info Abstract The Authors in Frontiers Rakesh Yadav Monika Maan Divya Yadav Google Rakesh Yadav Monika Maan Divya Yadav Google Scholar Rakesh Yadav Monika Maan Divya Yadav PubMed Rakesh Yadav Monika Maan Divya Yadav Related Article in Frontiers Google Scholar PubMed Abstract Close Back to top Javascript is disabled. Please enable Javascript in your browser settings in order to see all the content on this page.