Affiliations 

  • 1 College of Natural Science, Department of Biological Sciences, Kongju National University, Gongju, 32588, South Korea; Department of Chemistry, Government College University, Lahore, 54000, Pakistan. Electronic address: abbasi@gcu.edu.pk
  • 2 College of Natural Science, Department of Biological Sciences, Kongju National University, Gongju, 32588, South Korea
  • 3 Department of Chemistry, Government College University, Lahore, 54000, Pakistan
  • 4 Faculty of Pharmacy and Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Level 9, FF3, Universiti Teknologi MARA, Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia
  • 5 Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur, 63100, Pakistan
  • 6 Department of Biochemistry, University of Agriculture, Faisalabad, 38040, Pakistan
  • 7 College of Natural Science, Department of Biological Sciences, Kongju National University, Gongju, 32588, South Korea. Electronic address: dnalove@kongju.ac.kr
Comput Biol Chem, 2018 Dec;77:72-86.
PMID: 30245349 DOI: 10.1016/j.compbiolchem.2018.09.007

Abstract

The heterocyclic compounds have been extensively reported for their bioactivity potential. The current research work reports the synthesis of some new multi-functional derivatives of 2-furoic piperazide (1; 1-(2-furoyl)piperazine). The synthesis was initiated by reacting the starting compound 1 with 3,5-dichloro-2-hydroxybenzenesulfonyl chloride (2) in a basic, polar and protic medium to obtain the parent sulfonamide 3 which was then treated with different electrophiles, 4a-g, in a polar and aprotic medium to acquire the designed molecules, 5a-g. These convergent derivatives were evaluated for their inhibitory potential against α-glucosidase, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Acarbose was used as a reference standard for α-glucosidase inhibition while eserine for AChE and BChE inhibition. Some of the synthesized compounds were identified as promising inhibitors of these three enzymes and their bioactivity potentials were also supported by molecular docking study. The most active compounds among the synthetic analogues might be helpful in drug discovery and development for the treatment of type 2 diabetes and Alzhiemer's diseases.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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