Synthesis, characterization and enzyme inhibition study of O-substituted derivatives of chlorinated coumarin

Journal Title: Pakistan Journal of Pharmaceutical Sciences - Year 2014, Vol 27, Issue 2

Abstract

 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.

Authors and Affiliations

Aziz-ur-Rehman , Sehreen Magsi , Muhammad Athar Abbasi , Shahid Rasool , Abdul Malik , Ghulam Hussain , Muhammad Ashraf , Noreen Khalid

Keywords

Related Articles

 Taguchi’s experimental design for optimizing the production of novel thermostable polypeptide antibiotic from Geobacillus pallidus SAT4

 Polypeptide antimicrobials used against topical infections are reported to obtain from mesophilic bacterial species. A thermophilic Geobacillus pallidus SAT4 was isolated from hot climate of Sindh Dessert, Pakistan...

 Induction of heme oxygenase-1 attenuates chemotherapy-induced pulmonary toxicity in rats: A possible link between heme oxygenase-1 and NF-κB

 A critical restriction in the use of bleomycin (BLM) is development of pulmonary fibrosis via oxidative and inflammatory mechanisms. Drugs that induce heme oxygenase-1 (HO-1) like hemin (HEM), have anti-inflammator...

 Enhanced Ehrlich tumor inhibition using DOX-NP and gold nanoparticles loaded liposomes

 Treatment with doxorubicin (DOX) is a common treatment for different types of cancer. DOX-NP is one of a well established marketed liposomal formulation for DOX. It has advantages over free DOX in reducing the card...

 Bioremediation of petroleum hydrocarbon contaminated soil by Rhodobacter sphaeroides biofertilizer and plants

 Bio-augmentation is a promising technique for remediation of polluted soils. This study aimed to evaluate the bio-augmentation effect of Rhodobacter sphaeroides biofertilizer (RBF) on the bioremediation of total pe...

Interaction study of moxifloxacin and lomefloxacin with co-administered drugs

Moxifloxacin and lomefloxacin are fluoroquinolone antibiotics used in treating urinary and respiratory tract infections. Fluoroquinolones are known to have interactions with drugs that are active in gastro intestinal tra...

Download PDF file
  • EP ID EP88210
  • DOI -
  • Views 84
  • Downloads 0

How To Cite

Aziz-ur-Rehman, Sehreen Magsi, Muhammad Athar Abbasi, Shahid Rasool, Abdul Malik, Ghulam Hussain, Muhammad Ashraf, Noreen Khalid (2014).  Synthesis, characterization and enzyme inhibition study of O-substituted derivatives of chlorinated coumarin. Pakistan Journal of Pharmaceutical Sciences, 27(2), 271-278. https://europub.co.uk/articles/-A-88210