Affiliations 

  • 1 Department of Chemistry, Government College University Lahore 54000 Pakistan abbasi@gcu.edu.pk (+92)-42-111000010 Ext. 266
  • 2 Department of Biological Sciences, College of Natural Sciences, Kongju National University Gongju 32588 South Korea
  • 3 The Steve and Cindy Rasmussen Institute for Genomic Medicine, Nationwide Children Hospital Columbus Ohio 43205 USA
  • 4 Faculty of Pharmacy, Universiti Teknologi MARA Cawangan Selangor Kampus Puncak Alam Bandar Puncak Alam Selangor 42300 Malaysia
  • 5 Department of Biochemistry, University of Agriculture Faisalabad 38040 Pakistan
RSC Adv, 2024 May 15;14(23):16546-16559.
PMID: 38774615 DOI: 10.1039/d4ra01063a

Abstract

By using a convergent methodology, a unique series of N-arylated 4-yl-benzamides containing a bi-heterocyclic thiazole-triazole core was synthesized and the structures of these hybrid molecules, 9a-k, were corroborated through spectral analyses. The in vitro studies of these multi-functional molecules demonstrated their potent mushroom tyrosinase inhibition relative to the standard used. The kinetics mechanism was exposed by lineweaver-burk plots which revealed that, 9c, inhibited mushroom tyrosinase non-competitively by forming an enzyme-inhibitor complex. The inhibition constant Ki calculated from Dixon plots for this compound was 0.016 μM. The computational study was also consistent with the experimental results and these molecules disclosed good results of all scoring functions and interactions, which suggested a good binding to mushroom tyrosinase. So, it was predicted from the inferred results that these molecules might be considered as promising medicinal scaffolds for the diseases associated with the over-expression of this enzyme.

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

Similar publications