Lipophilicity Study of Thiazolo[3,2-a]pyrimidine Derivatives as Potential Bioactive Agents

AUTOR(ES)

Studzińska, Renata, Kołodziejska, Renata, Redka, Małgorzata, Modzelewska-Banachiewicz, Bożena, Augustyńska, Beata

FONTE

J. Braz. Chem. Soc.

DATA DE PUBLICAÇÃO

2016-09

RESUMO

Systems containing fused thiazole and pyrimidine rings play a significant role in organisms due to their biological activity. Lipophilicity, as important parameter to expect biological activity of the compounds, was evaluated for 27 potentially active thiazolo[3,2-a]pyrimidine derivatives using chromatographic methods: reversed phase thin layer chromatography (RP-TLC) and reversed phase high performance liquid chromatography (RP-HPLC) methods. Methanol was used as the organic modifier of the mobile phases. The corresponding relationship between compound's structure and lipophilicity parameters (RM0 and log kw) values were observed and featured. RM0 and log kw parameters were compared with computed log P values. For all of analyzed compounds, determined lipophilicity's parameters values are > 0 which means that there are hydrophobic substances, soluble in the lipid phase. Simultaneously, these values are < 5, i.e., are in accordance with Lipinski's rule in the range of lipophilicity. In the case of the possibility of their use as drugs, they will be active after oral application.

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