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Updated: Jun 16, 2026

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Published on: November 1, 2024
Potent oxadiazole CGRP receptor antagonists for the potential treatment of migraine
Paula L Nichols1, Jonathan Brand, Michael Briggs
1Department of Medicinal Chemistry, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. paula.l.nichols@gsk.com
Abstract:
A pharmacophore model was built, based on known CGRP receptor antagonists, and this was used to aid the identification of novel leads. Analogues were designed, modelled and synthesised which incorporated alternative 'LHS' fragments linked via either an amide or urea to a privileged 'RHS' fragment commonly found in CGRP receptor antagonists. As a result a novel series of oxadiazole CGRP receptor antagonists has been identified and the subsequent optimisation to enhance both potency and bioavailability is presented.
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