Next Article in Journal
Preparation and Quality Control of the [153Sm]-Samarium Maltolate Complex as a Lanthanide Mobilization Product in Rats
Previous Article in Journal
Models for the Prediction of Receptor Tyrosine Kinase Inhibitory Activity of Substituted 3-Aminoindazole Analogues
Article Menu

Article Versions

Export Article

Open AccessArticle
Sci. Pharm. 2011, 79(2), 259-264; doi:10.3797/scipharm.1012-20

Chemical Stability of New Acyclovir Analogues with Peptidomimetics

Department of Chemistry, South-West University 'Neofit Rilski', Ivan Michailov str. 66, 2700 Blagoevgrad, Bulgaria
*
Author to whom correspondence should be addressed.
Received: 20 December 2010 / Accepted: 3 March 2011 / Published: 5 March 2011
Download PDF [181 KB, uploaded 26 September 2016]

Abstract

In the search for new and effective prodrugs against the herpes simplex virus, a series of acyclovir analogues with a thiazole ring containing amino acids (glycine, alanine, valine, leucine) has been investigated. The chemical stability of some of the compounds containing different residues was studied at pH 1 and pH 7.4 at a temperature of 37°C. An HPLC method was developed for quantification of the unchanged ester concentration. Some of the esters (Gly-thiazole, Ala-thiazole-acyclovir, Leu-thiazole-acyclovir) were rather unstable, especially under acidic conditions, and underwent rapid hydrolysis into the chemical precursor acyclovir. At pH 7.4, the stability of Valthiazole- acyclovir was remarkable. At this pH, Val-thiazole-acyclovir showed stability higher than that of valacyclovir (the first effective prodrug of acyclovir).
Keywords: Amino acids; Thiazole; Antiviral drugs; HPLC; Prodrugs Amino acids; Thiazole; Antiviral drugs; HPLC; Prodrugs
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

HRISTOV, G.; STANKOVA, I. Chemical Stability of New Acyclovir Analogues with Peptidomimetics. Sci. Pharm. 2011, 79, 259-264.

Show more citation formats Show less citations formats

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Sci. Pharm. EISSN 2218-0532 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top