Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors
Graphical abstract
Phenanthrene imidazole 3 has been identified as a novel potent, selective, and orally active mPGES-1 inhibitor.
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2019, Prostaglandins and Other Lipid MediatorsCitation Excerpt :A variety of structurally different mPGES-1 inhibitors were developed; phenanthrene imidazoles, 2,4-biarylimidazoles, trisubstituted urea derivatives, dioxobenzo-thiazinones, benzoxazoles, imidazoquinolines. Indeed, some of them can significantly inhibit human mPGES-1 with IC50 values in the single-digit nanomolar or even subnanomolar range [28–31]. Noticeably, most of mPGES-1 inhibitors have partial or no activity on rodent mPGES-1, which impose restrictions on using the well-established mouse/rat models of inflammation-related diseases for preclinical studies [32,33].