Abstract
A series of new peptidomimetics based on the tripeptide sequence Z-Leu-Phe-Gln-OH were synthesized, with ten of these including the α-nitrogen atom of the N-terminal amino acid incorporated into the pyrrole cycle. The synthesized compounds were tested for antiviral activity by agar-diffusion plaque inhibition test against Coxsackievirus B1 replication in FL cell. Four of the products were observed to possess an antiviral activity, which was proven to be significant for one product. N- terminal pyrrole moiety and C-terminal free carboxyl function are available in all active compounds. On the other hand, their corresponding -OBzl and -OBut esters are inactive.
Keywords: Antipicornaviral compounds, pyrroles, peptidomimetics, 3C inhibitors, Coxsackievirus, SPPS
Protein & Peptide Letters
Title: Design, Synthesis and Biological Evaluation of Antipicornaviral Pyrrole-Containing Peptidomimetics
Volume: 14 Issue: 9
Author(s): I. Minchev, S. Vladimirova, L. Vezenkov, A. Bijev, V. Moussis, L. Nikolaeva-Glomb, V. Tsikaris, M. Czeuz and A. Galabov
Affiliation:
Keywords: Antipicornaviral compounds, pyrroles, peptidomimetics, 3C inhibitors, Coxsackievirus, SPPS
Abstract: A series of new peptidomimetics based on the tripeptide sequence Z-Leu-Phe-Gln-OH were synthesized, with ten of these including the α-nitrogen atom of the N-terminal amino acid incorporated into the pyrrole cycle. The synthesized compounds were tested for antiviral activity by agar-diffusion plaque inhibition test against Coxsackievirus B1 replication in FL cell. Four of the products were observed to possess an antiviral activity, which was proven to be significant for one product. N- terminal pyrrole moiety and C-terminal free carboxyl function are available in all active compounds. On the other hand, their corresponding -OBzl and -OBut esters are inactive.
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Cite this article as:
Minchev I., Vladimirova S., Vezenkov L., Bijev A., Moussis V., Nikolaeva-Glomb L., Tsikaris V., Czeuz M. and Galabov A., Design, Synthesis and Biological Evaluation of Antipicornaviral Pyrrole-Containing Peptidomimetics, Protein & Peptide Letters 2007; 14 (9) . https://dx.doi.org/10.2174/092986607782110220
DOI https://dx.doi.org/10.2174/092986607782110220 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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