3-(1-Aminoalkyl)pyrazole- and4,5-Dihydropyrazole-5-carboxylic Acids as Peptide Bond Replacements

doi:10.1055/S-0030-1259303

Paper

3-(1-Aminoalkyl)pyrazole- and4,5-Dihydropyrazole-5-carboxylic Acids as Peptide Bond Replacements

Published 2011 · Raymond C. F. Jones, L. E. Seager, M. Elsegood

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Abstract

Orthogonally protected 3-(1-aminoalkyl)pyrazole- and 4,5-dihydropyrazole-5-carboxylic acids are prepared by 1,3-dipolar cycloaddition of α-aminonitrile imines with electron-deficient alkenes ; the pyrazole is incorporated into pseudotri- and tetrapeptides.

Study Snapshot

Orthogonally protected 3-(1-aminoalkyl)pyrazole- and 4,5-dihydropyrazole-5-carboxylic acids can be used as peptide bond replacements in various peptide structures.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

3-(1-Aminoalkyl)pyrazole- and4,5-Dihydropyrazole-5-carboxylic Acids as Peptide Bond Replacements

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References

Citations

A base promoted multigram synthesis of aminoisoxazoles: valuable building blocks for drug discovery and peptidomimetics

This study developed a metal-free, base-promoted method for the synthesis of aminoisoxazoles, valuable building blocks for drug discovery and peptidomimetics.

Methodology for Synthesis of Enantiopure 3,5‐Disubstituted Pyrrol‐2‐ones

This study developed a new synthetic route towards chiral 3,5-disubstituted pyrrol-2-ones from amino acids, leading to a series of lactam analogues of antifungal 3-(aryl)-5-hydroxymethyl-2,5-dihydrofuran-2-

Pyrazoles as non-classical bioisosteres in prolylcarboxypeptidase (PrCP) inhibitors.

Pyrazoles are suitable bioisosteric replacements for amide functional groups in prolylcarboxypeptidase (PrCP) inhibitors, maintaining potency and minimizing adverse effects.