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۱Design and Synthesis of New Biarylhydrazides Possessing an Azido Pharmacophore as Selective COX–2 Inhibitors
اطلاعات انتشار: Journal of Pharmaceutical & Health Sciences، اول،شماره۴، ۲۰۱۲ autumn، سال
تعداد صفحات: ۶
A group of 1,3–biarylhydrazide derivatives possessing a COX–2 azido pharmacophore at the Para– position of the C–1 phenyl ring in conjunction with a N–3 phenyl or substituted–phenyl ring (4–F,4–Cl,4–OMe) were designed and synthesized based on nucleophilic substitution reaction. A molecular modelling study of these compounds showed that the designed molecules were well bound with the active site of COX–2 enzyme and the N3 pharmacophore was well oriented into the COX–2 secondary pocket. Thus, we expect the compounds show good potency and selectivity on COX–2 inhibition.
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