The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists
Bioorganic & Medicinal Chemistry Letters(2009)
Abstract
A series of tricyclic CGRP receptor antagonists was optimized in order to improve oral bioavailability. Attenuation of polar surface area and incorporation of a weakly basic indoline nitrogen led to compound 5, a potent antagonist with good oral bioavailability in three species.
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Key words
CGRP receptor antagonists,CGRP,Migraine,Orally bioavailable
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