Affiliations 

  • 1 Department of Chemistry, Government College University, Lahore-54000, Pakistan
  • 2 The Steve and Cindy Rasmussen Institute for Genomic Medicine, Nationwide Children Hospital, Columbus, Ohio, 43205, USA
  • 3 Department of Zoology, Mirpur University of Science and Technology (MUST), Mirpur, 10250 (AJK), Pakistan
  • 4 Department of Physiology & Biochemistry, Cholistan University of Veterinary and Animal Sciences, Bahawalpur, 63100, Pakistan
  • 5 Faculty of Pharmacy, Universiti Teknologi MARA Cawangan, Selangor Kampus Puncak Alam, Bandar Puncak Alam, 42300, Selangor, Malaysia
Chem Biodivers, 2024 Apr;21(4):e202400133.
PMID: 38363553 DOI: 10.1002/cbdv.202400133

Abstract

In the aimed research study, a new series of N-(aryl)-3-[(4-phenyl-1-piperazinyl)methyl]benzamides was synthesized, which was envisaged as tyrosinase inhibitor. The structures of these newly designed molecules were verified by IR, 1H-NMR, 13C-NMR, EI-MS and CHN analysis data. These molecules were screened against tyrosinase and their inhibitory activity explored that these 3-substituted-benzamides exhibit good to excellent potential, comparative to the standard. The Kinetics mechanism was investigated through Lineweaver-Burk plots which depicted that molecules inhibited this enzyme in a competitive mode. Moreover, molecular docking was also performed to determine the binding interaction of all synthesized molecules (ligands) with the active site of tyrosinase enzyme and the results showed that most of the ligands exhibited efficient binding energy values. Therefore, it is anticipated that these molecules might serve as auspicious therapeutic scaffolds for treatment of the tyrosinase associated skin disorders.

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

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