Lipophilic Character of Novel Amino Acid Derivatives of Zidovudine with Anti HIV Activity

MORONI, G.N.; QUEVEDO, M.A.; RAVETTI, S.A.; BRIÑÓN, M.C.

JOURNAL OF LIQUID CHROMATOGRAPHY AND RELATED TECHNOLOGIES

Marcel Dekker

Lugar: New York; Año: 2002 vol. 25 p. 1345 - 1345

1082-6076

p class="MsoNormal" style="MARGIN: 0cm 0cm 0pt; TEXT-ALIGN: justify; mso-layout-grid-align: none">The lipophilic properties of a novel series of zidovudine amino acid derivatives were measured using chromatographic techniques, reversed-phase thin layer chromatography (RP-TLC) and reversed-phase high performance liquid chromatography (RP-HPLC), as well as the classic shake flask (log Po/w) and theoretical CLOGP methods. These novel derivatives, obtained by association of zidovudine (AZT) with the essential amino acids leucine (AZT-Leu), isoleucine (AZT-iLeu), phenylalanine (AZT-Phe), valine (AZT-Val), proline (AZT-Prol) and tryptophane (AZT-Tryp), exhibited an increased log Po/w, as compared with the parent compound as follows: AZT-iLeu > AZT-Leu