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

Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Articles in this Issue were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence. Articles are hosted by MDPI on as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).
Open AccessArticle
Sci. Pharm. 2011, 79(2), 259-264; (registering DOI)

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
PDF [181 KB, uploaded 26 September 2016]


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).

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



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