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Novel oxazolidinone calcitonin gene-related peptide (CGRP) receptor antagonists for the acute treatment of migraine.

Abstract：

:In our efforts to develop CGRP receptor antagonists as backups to MK-3207, 2, we employed a scaffold hopping approach to identify a series of novel oxazolidinone-based compounds. The development of a structurally diverse, potent (20, cAMP+HS IC50=0.67 nM), and selective compound (hERG IC50=19 μM) with favorable rodent pharmacokinetics (F=100%, t1/2=7h) is described. Key to this development was identification of a 3-substituted spirotetrahydropyran ring that afforded a substantial gain in potency (10 to 35-fold).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Crowley BM,Stump CA,Nguyen DN,Potteiger CM,McWherter MA,Paone DV,Quigley AG,Bruno JG,Cui D,Culberson JC,Danziger A,Fandozzi C,Gauvreau D,Kemmerer AL,Menzel K,Moore EL,Mosser SD,Reddy V,White RB,Salvatore CA,Kane S

doi

10.1016/j.bmcl.2015.07.021

subject

Has Abstract

pub_date

2015-11-01 00:00:00

pages

4777-4781

issue

21

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)00725-8

journal_volume

25

pub_type

杂志文章

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