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Substituted imidazoles as glucagon receptor antagonists. 2001
L L Chang, and
K L Sidler, and
M A Cascieri, and
S de Laszlo, and
G Koch, and
B Li, and
M MacCoss, and
N Mantlo, and
S O'Keefe, and
M Pang, and
A Rolando, and
W K Hagmann
Department of Medicinal Chemical Research, Merck Research Laboratories, Rahway, NJ 07065, USA. linda_chang@merck.com
A modestly active, nonselective triarylimidazole lead was optimized for binding affinity with the human glucagon receptor. This led to the identification of a 2- and/or 4-alkyl or alkyloxy substituent on the imidazole C4-aryl group as a structural determinant for significant enhancement in binding with the glucagon receptor (e.g., 41, IC(50)=0.053 microM) and selectivity (>1000x) over p38MAP kinase in this class of compounds.
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S de Laszlo, and
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M Pang, and
A Rolando, and
W K Hagmann
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S O'Keefe, and
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K L Sidler, and
M A Cascieri, and
S de Laszlo, and
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M MacCoss, and
N Mantlo, and
S O'Keefe, and
M Pang, and
A Rolando, and
W K Hagmann
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