| Title : Potent benzimidazolone-based CGRP receptor antagonists - Theberge_2008_Bioorg.Med.Chem.Lett_18_6122 |
| Author(s) : Theberge CR , Bednar RA , Bell IM , Corcoran HA , Fay JF , Hershey JC , Johnston VK , Kane SA , Mosser S , Salvatore CA , Williams TM , Zartman CB , Zhang XF , Graham SL , Vacca JP |
| Ref : Bioorganic & Medicinal Chemistry Lett , 18 :6122 , 2008 |
|
Abstract :
The previously disclosed spirohydantoin-based CGRP receptor antagonists were optimized for potency through modification of the benzimidazolone substituents. Compounds were identified which had minimal shift in the cAMP functional assay containing 50% human serum. Blockade of CGRP-mediated vasodilation was observed with these compounds in a rhesus pharmacodynamic assay and the in vivo potency correlated with the in vitro activity in the serum-shifted functional assay. |
| PubMedSearch : Theberge_2008_Bioorg.Med.Chem.Lett_18_6122 |
| PubMedID: 18947992 |
Theberge CR, Bednar RA, Bell IM, Corcoran HA, Fay JF, Hershey JC, Johnston VK, Kane SA, Mosser S, Salvatore CA, Williams TM, Zartman CB, Zhang XF, Graham SL, Vacca JP (2008)
Potent benzimidazolone-based CGRP receptor antagonists
Bioorganic & Medicinal Chemistry Lett
18 :6122
Theberge CR, Bednar RA, Bell IM, Corcoran HA, Fay JF, Hershey JC, Johnston VK, Kane SA, Mosser S, Salvatore CA, Williams TM, Zartman CB, Zhang XF, Graham SL, Vacca JP (2008)
Bioorganic & Medicinal Chemistry Lett
18 :6122