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Synthesis of Mefenamic Acid Containing N ‐Glycoconjugates and Their Evaluation as Human COX‐2 Enzyme Inhibitor
Author(s) -
Madduluri Vimal K.,
Sah Ajay K.
Publication year - 2020
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201904655
Subject(s) - mefenamic acid , enzyme , chemistry , acute toxicity , biochemistry , protein data bank (rcsb pdb) , pharmacology , glycoconjugate , in vitro , enzyme assay , toxicity , biology , chromatography , organic chemistry
A series of d ‐glucose derived N ‐glycopeptides containing mefenamic acid have been synthesised and in vitro evaluation of all these molecules have been performed as COX‐2 (human) enzyme inhibitor using Enzymes Immuno Assay kit. These studies were further supported by docking experiments on human COX‐2 enzyme (PDB ID: 5IKR). All the compounds exhibited a fair amount of COX‐2 enzyme inhibition during both the modes of study and tryptophan derivative showed the best activity. Acute toxicity (LD 50 ) in rat has also been evaluated using General Unrestricted Structure‐Activity Relationships (GUSAR) software, where acute oral toxicity for most of the molecules was found to be less than the pure mefenamic acid.