Bioorganic and Medicinal Chemistry Letters 2012-Apr
Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group.
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概要
In our continuing efforts to identify CGRP receptor antagonists that can be dosed orally for the treatment of migraine headache, we have investigated a pyridine bioisosteric replacement of a polar amide portion of a previous lead compound, BMS-694153. Pyridine derivatives were discovered and their SAR was studied. Some of them showed excellent binding potency. However, oral bioavailability was low, even for compounds with good Caco-2 cell permeability.
