- Rhodanineacetic acid derivatives as potential drugs: Preparation, hydrophobic properties and antifungal activity of (5-arylalkylidene-4-oxo-2- thioxo-1,3-thiazolidin-3-yl)acetic acids
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Some [(5Z)-(5-arylalkylidene-4-oxo-2-thioxo-1,3-thiazolidin-3-yl)]acetic acids were prepared as potential antifungal compounds. The general synthetic approach to all synthesized compounds is presented. Lipophilicity of all the discussed rhodanine-3-acetic acid derivatives was analyzed using a reversed phase high performance liquid chromatography (RP-HPLC) method. The procedure was performed under isocratic conditions with methanol as an organic modifier in the mobile phase using an end-capped non-polar C18 stationary RP column. The RP-HPLC retention parameter log k (the logarithm of the capacity factor k) is compared with log P values calculated in silico. All compounds were evaluated for antifungal effects against selected fungal species. Most compounds exhibited no interesting activity, and only {(5Z)-[4-oxo-5-(pyridin-2- ylmethylidene)-2-thioxo-1,3-thiazolidin-3-yl]}acetic acid strongly inhibited the growth of Candida tropicalis 156, Candida krusei E 28, Candida glabrata 20/Iand Trichosporon asahii 1188.
- Dolezel, Jan,Hirsova, Petra,Opletalova, Veronika,Dohnal, Jiri,Marcela, Vejsova,Kunes, Jiri,Jampilek, Josef
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experimental part
p. 4197 - 4212
(2010/03/03)
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- Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient
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The rhodanine derivatives of the general formula: STR1 wherein (I) R1 and R2 are taken together to represent a tetramethylene or pentamethylene group; (II) R1 represents a hydrogen atom, and R2 represents (1) a
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