Abstract
In the course of our program for discovery of novel DPP-IV inhibitors, a series of pyrazolo[1,5-a]pyrimidines were found to be novel DPP-IV inhibitors. We identified N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (4a) and described its pharmacological profiles.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Dipeptidyl Peptidase 4 / metabolism
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Dipeptidyl-Peptidase IV Inhibitors / chemistry
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Dipeptidyl-Peptidase IV Inhibitors / pharmacokinetics
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Dipeptidyl-Peptidase IV Inhibitors / pharmacology*
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Dogs
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Humans
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Male
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Pyrimidines / administration & dosage
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Pyrimidines / chemistry
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Pyrimidines / pharmacokinetics
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Pyrimidines / pharmacology*
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Pyrimidines / therapeutic use
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Rats
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Rats, Sprague-Dawley
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Rats, Wistar
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Structure-Activity Relationship
Substances
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Dipeptidyl-Peptidase IV Inhibitors
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Pyrimidines
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Dipeptidyl Peptidase 4
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anagliptin