Calculation procedures and HPLC method for analysis of the lipophilicity of acyclovir esters |
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| Authors: | Monika A Lesniewska Zofia Gdaniec |
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| Affiliation: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Poznan University of Medical Sciences, Poznan, Poland and;2. Institute of Bioorganic Chemistry, Polish Academy of Sciences, Poznan, Poland |
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| Abstract: | Acyclovir (ACV) belongs to a class of drugs with low bioavailability. Selected ACV esters including acetyl (Ac-), isobutyryl (iBut-), pivaloyl (Piv-), ethoxycarbonyl (Etc-) and nicotinoyl (Nic-) were synthesized, and their lipophilicity was determined by the high-performance liquid chromatography (HPLC) RP method. Statistical analyses of the comparative values of log?P and clog?P were carried out using computational methods. It was proved that the AC log?P algorithm can be useful for the analysis of these compounds and has a statistically justified application in the assessment of the quantitative structure–activity relationship. Moreover, the lipophilicity determined by the HPLC method appears as follows: ACV?
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| Keywords: | Acyclovir antiviral calculated log?P HPLC lipophilicity |
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