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Matches in SemOpenAlex for { <https://semopenalex.org/work/W2010308260> ?p ?o ?g. }

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• W2010308260 abstract "Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Replacements for the benzodiazepine core of an earlier lead structure 1 including 5-, 6-, and 7-membered lactams were explored. Within the 7-membered ring scaffold, phenyl substitution at various positions afforded the potent (3R)-amino-(6S)-phenyl caprolactam template. The phenylimidazolinone privileged structure gave additional potency enhancements, as 24 showed good potency in both CGRP binding (Ki = 2 nM) and cAMP (IC50 = 4 nM) assays and was orally bioavailable in rats (27%)." @default.
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• W2010308260 date "2007-09-01" @default.
• W2010308260 modified "2023-10-04" @default.
• W2010308260 title "Caprolactams as potent CGRP receptor antagonists for the treatment of migraine" @default.
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• W2010308260 doi "https://doi.org/10.1016/j.bmcl.2007.06.062" @default.
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