Tuberculosis (TB), since the introduction to the therapy streptomycin and other several anti-TB agents, is curable disease. However, nowadays it is estimated that one third of the world's population is infected with TB which could progress to active disease within their lifetime. It is also observed the development of "drug resistance" forms of the disease (especially "multi-drug resistant" TB). That is why the new selective anti-TB drugs are necessary [1].

Lipophilicity (log P), one of the factors determinating the amount of drug reaching the place of its action, can be evaluated by the traditional "shake-flask" method or by chromatographic techniques (RP-HPLC or RP-TLC). Reversed phase thin layer chromatography (RP-TLC) is very convenient and speed method for use.

The tested 5-arylidene-(thio)hydantoin derivatives showed different in vitro activity against Mycobacterium tuberculosis from 0% to 97% inhibition as reported earlier [2, 3].

Lipophilicity of these compounds and TB-drugs (Isoniazid and Thioacetazone) was evaluated on silica gel RP-18 F_254s plates. A mixture of acetone and water with acetone content in the range 60-80% were used as mobile phase. The values of the experimental lipophilicity R_M0 for hydantoin derivatives were in the ranges 2.475 to 4.263 and much lower for Isoniazid (1.273) and Thioacetazone (0.667).

The partition coefficient log P was also calculated by means of computer programs (exp. KnowWin, ClogP, Interactive analysis, ChemDraw and Ched). The calculated values of lipophilicity (log P_cal) were mostly lower than the experimental R_M0 values.

[1] www.taccf.org

[2] Kieć-Kononowicz, K.; Szymańska, E. Il Farmaco (2002) 57, 909-916.

[3] Kieć-Kononowicz, K.; Szymańska, E. The fourth Mulidisciplinary Conference on Drug Research, Gdańsk-Sobieszewo, 17-19 maja 2004, P-36.

This work was partly supported by grant no. BBN 501/P/185/F.

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