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Synthesis, characterization and enzyme inhibition study of O-substituted derivatives of chlorinated Coumarin.
Author(s)
Aziz-Ur-Rehman Department of Chemistry, Government College University, Lahore, Pakistan
Sehreen Magsi Department of Chemistry, Government College University, Lahore, Pakistan
Muhammad Athar Abbasi Department of Chemistry, Government College University, Lahore, Pakistan
Shahid Rasool Department of Chemistry, Government College University, Lahore, Pakistan
Abdul-Malik HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Pakistan
Ghulam-Hussain Department of Chemistry, Government College University, Lahore, Pakistan
Muhammad Ashraf Department of Biochemistry & Biotechnology, The Islamia University of Bahawalpur, Pakistan
Noreen Khalid Department of Pharmacy, The Islamia University of Bahawalpur, Pakistan
Abstract
Coumarins have much importance in dyes, drugs, perfumes and pesticides. In the demonstrated research work, a benignant series of chlorinated coumarins was synthesized and screened against different enzymes. First, 6-Chloro-7- hydroxy-4-methyl-2H-chromen-2-one (3) was geared up by the reaction of 4-chlororesorcinol (1) and ethyl acetoacetate (2) in the presence of concentrated H2SO4. Second, various O-substituted derivatives of chlorinated coumarins, 5a-j, were set up by pairing different alkyl/aralkyl halides, 4a-j, with 3 in the presence of NaH in DMF as solvent. The structures of all the synthesized compounds were clarified through spectral analysis using EI-MS, IR and 1H-NMR. The different enzymes used for the evaluation of bioactivity of all the synthesized compounds were acetyl cholinesterase (AChE), butyryl cholinesterase (BChE) and lipoxygenase (LOX). The most proficient activity was shown against both cholinesterase enzymes.
Publication Details
Page(s) 271-278
DOI DOI not available
Published Journal: Pakistan Journal of Pharmaceutical Sciences, Volume: 27, Issue: 2, Year: 2014
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