Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead

Theresa M. Williams,Craig A. Stump,Diem N. Nguyen,Amy G. Quigley,Ian M. Bell,Steven N. Gallicchio,C. Blair Zartman,Bang-Lin Wan,Kimberly Della Penna,Priya Kunapuli,Stefanie A. Kane,Ken S. Koblan,Scott D. Mosser,Ruth Z. Rutledge,Christopher Salvatore,John F. Fay,Joseph P. Vacca,Samuel L. Graham

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

Structure activity studies led to the non-peptide CGRP antagonist, 7 (Ki=44nM, IC50=38nM), which was orally bioavailable in rats. Benzodiazepinone 7 is a promising new lead in the development of orally bioavailable CGRP antagonists for the treatment of migraine.

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关键词

CGRP receptor antagonist,Benzodiazepinone,CGRP,CLR/RAMP1,Migraine

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