Potent oxadiazole CGRP receptor antagonists for the potential treatment of migraine.


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.

DOI: 10.1016/j.bmcl.2010.01.012

Cite this paper

@article{Nichols2010PotentOC, title={Potent oxadiazole CGRP receptor antagonists for the potential treatment of migraine.}, author={Paula L Nichols and Jonathan Brand and Michael A Briggs and Mathilde D'Angeli and Jennifer Farge and S. L. Garland and Paul A Goldsmith and Rio Hutchings and Ian R Kilford and Ho Yin Li and David MacPherson and Fiona Nimmo and Francis Dominic Sanderson and Sanjeet S Sehmi and Nicola Shuker and John Skidmore and Michael Stott and Jennifer A Sweeting and Hasmi Tajuddin and Andrew K. Takle and Giancarlo Trani and Ian D. Wall and Robert W Ward and David M. Wilson and David R Witty}, journal={Bioorganic & medicinal chemistry letters}, year={2010}, volume={20 4}, pages={1368-72} }