Abstract
A new series of DPP-4 inhibitors derived from piperidine-fused benzimidazoles and imidazopyridines is described. Optimization of this class of DPP-4 inhibitors led to the discovery of imidazopyridine 34. The potency, selectivity, cross-species DMPK profiles, and in vivo efficacy of 34 is reported.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Animals
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Benzimidazoles / chemical synthesis
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Benzimidazoles / pharmacology
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Chemistry, Pharmaceutical / methods*
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Crystallography, X-Ray / methods
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Dipeptidyl-Peptidase IV Inhibitors / chemical synthesis*
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Dipeptidyl-Peptidase IV Inhibitors / pharmacology
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Dogs
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Drug Design
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Glucagon-Like Peptide 1 / chemistry
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Humans
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Hydrolysis
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Imidazoles / chemical synthesis*
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Imidazoles / pharmacology
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Inhibitory Concentration 50
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Macaca mulatta
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Mice
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Piperidines / chemical synthesis*
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Piperidines / chemistry*
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Piperidines / pharmacology
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Pyrazines / chemical synthesis
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Pyrazines / pharmacology
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Pyridines / chemical synthesis
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Pyridines / pharmacology
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Rats
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Sitagliptin Phosphate
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Triazoles / chemical synthesis
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Triazoles / pharmacology
Substances
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Benzimidazoles
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Dipeptidyl-Peptidase IV Inhibitors
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Imidazoles
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Piperidines
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Pyrazines
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Pyridines
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Triazoles
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Glucagon-Like Peptide 1
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benzimidazole
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Sitagliptin Phosphate