SYNTHESIS AND STABILITY STUDY ON AN ASPIRIN DERIVATIVE WITH POTENTIAL SELECTIVE COX-2 INHIBITOR

Document Type : Original Article

Authors

1 Department of medicinal chemistry

2 Faculty of Pharmacy, Sana'a University

Abstract

       The synthesis of N– [5– Methyl– 2– (1, 3, 4 COX-2 selective inhibitor and the preliminary kinetic study for hydrolysis of this compound is studied in this paper. The compound was prepared from the corresponding aspirin and 2–amino–5–methyl–1,3,4–thiadiazole in the presence of N,N-dicyclohexylcarbodiimide (DCC) as coupling agent .
       The preliminary kinetic study for hydrolysis of this compound and the effect of pH on the rate of hydrolysis in buffer solution citrate–phosphate–borate/HCl was studied. The structure was confirmed by infrared, nuclear magnetic resonance (H–NMR), and elemental microanalysis assay. The compound underwent slightly hydrolysis at low and high pH with a fairly stabile so, provide a chance for it to be absorbed intact with highly bioavailability, longer half life, and with lower G1 toxicity.