Abstract
The synthesis and structure-activity relationships of novel dipeptidyl peptidase IV inhibitors replacing the classical cyanopyrrolidine P1 group with other small nitrogen heterocycles are described. A unique potency enhancement was achieved with beta-branched natural and unnatural amino acids, particularly adamantylglycines, linked to a (2S,3R)-2,3-methanopyrrolidine based scaffold.
Publication types
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Comparative Study
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Validation Study
MeSH terms
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Dipeptides / chemistry*
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Dipeptides / pharmacology
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Dipeptidyl-Peptidase IV Inhibitors* / chemistry*
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Dipeptidyl-Peptidase IV Inhibitors* / pharmacology
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Drug Evaluation, Preclinical
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Humans
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Nitriles / chemistry
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Nitriles / pharmacology
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Structure-Activity Relationship
Substances
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Dipeptides
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Dipeptidyl-Peptidase IV Inhibitors
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Nitriles