Synthesis, Characterization and Anti-Inflammatory Study of New Heterocyclic Coumarin Derivatives
Keywords:Heterocyclic coumarin derivatives, anti-inflammatory, selective COX-2 inhibitor
The inflammation is one of the most central processes in animal cells defense versus certain injuries or
infections of microbes. The most essential metabolic precursor for many inflammatory pathways is PGH2
(prostaglandin), which catalytic synthesis from the AA (arachidonic acid) by COX enzymes. COX can be
divided in to three isomer COX-1 has important role in many physiological function like hemostasis, platelet
aggregation, and protection of gastric mucosa, COX-2 when stimulate cause formation of PGE2 excessively,
with other prostaglandin then decrease the pain threshold and nerve ending sensitization, which induce
pain, increase permeability of vascular and then enhance the inflammatory associated diseases pathway, and
COX-3 has special characteristic, its higher sensitivity to acetaminophen and present in brain. The NSAIDs
are therapeutic agents used for the treatment of inflammation, pain, and fever, they work by decreasing the
production of prostaglandins due to inhibiting the function of the cyclooxygenase (COX) enzyme, we have
two types nonselective and selective COX-2 inhibitors. In order to design new agents with no or low side
effect, the COX-2 selectivity should be increased, this achieved by design molecule structurally similar to
approved selective COX-2 inhibitors. The synthetic compound in this study contain three pharmacophores,
a nucleus of coumarin and substituted oxazole moiety, separated by a hydrazonoethyl spacer, which have
structural similarity properties to selective COX-2 inhibitors.
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