Chemical Stability of New Acyclovir Analogues with Peptidomimetics
AbstractIn 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).
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HRISTOV, G.; STANKOVA, I. Chemical Stability of New Acyclovir Analogues with Peptidomimetics. Sci. Pharm. 2011, 79, 259-264.
HRISTOV G, STANKOVA I. Chemical Stability of New Acyclovir Analogues with Peptidomimetics. Scientia Pharmaceutica. 2011; 79(2):259-264.Chicago/Turabian Style
HRISTOV, Georgi; STANKOVA, Ivanka. 2011. "Chemical Stability of New Acyclovir Analogues with Peptidomimetics." Sci. Pharm. 79, no. 2: 259-264.