Abstract

We describe a series of pyrazole and isoxazole analogs as antagonists of the α vβ 3 receptor. Compounds showed low to sub-nanomolar potency against α vβ 3, as well as good selectivity against α IIbβ 3. In HT29 cells, most analogs also demonstrated significant selectivity against α vβ 6. Several compounds showed good pharmacokinetic properties in rats, in addition to anti-angiogenic activity in a mouse corneal micropocket model. Compounds were synthesized in a straightforward manner from readily available glutarate precursors.

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