Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 16, Pages 4858-4861Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm800546t
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Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Early chemistry leads suffered from modest potency, significant CYP3A4 inhibition, and poor aqueous solubility. Herein. we describe the optimization of these leads to give 4 (BMS-694153), a molecule with outstanding potency, a favorable predictive toxicology profile, and remark-able aqueous solubility. Compound 4 has good intranasal bioavailablity in rabbits and shows close-dependent activity in validated in vivo and ex vivo migraine models.
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