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Proučavanje lipofilnosti potencijalno biološki aktivnih derivata cijanoacetamida

2017; Volume: 9; Issue: 1 Linguagem: Inglês

10.7251/jepm1709001a

ISSN

2566-3615

Autores

Suzana Apostolov, Gyöngyi Vastag,

Tópico(s)

Steroid Chemistry and Biochemistry

Resumo

<p><span style="color: rgba(0, 0, 0, 0.87); font-family: 'Noto Sans', -apple-system, BlinkMacSystemFont, 'Segoe UI', Roboto, Oxygen-Sans, Ubuntu, Cantarell, 'Helvetica Neue', sans-serif;">By applying the Lipinski’s rule for selected cyanoacetamide derivatives the possible existence of biological activity is theoretically investigated. Alos,using appropriate software packages and applying reverse-phase thin-layer chromatography (RP TLC18 F</span><span style="font-size: 10.5px; line-height: 0; position: relative; vertical-align: baseline; bottom: -0.25em; color: rgba(0, 0, 0, 0.87); font-family: 'Noto Sans', -apple-system, BlinkMacSystemFont, 'Segoe UI', Roboto, Oxygen-Sans, Ubuntu, Cantarell, 'Helvetica Neue', sans-serif;">254s</span><span style="color: rgba(0, 0, 0, 0.87); font-family: 'Noto Sans', -apple-system, BlinkMacSystemFont, 'Segoe UI', Roboto, Oxygen-Sans, Ubuntu, Cantarell, 'Helvetica Neue', sans-serif;">) in water-t-butanol, water-dimethylformamide and water-dimethylsulfoxide the lipophilicity of the studied cyanoacetamides was determined. Chromatographic retention parameters, RM</span><span style="font-size: 10.5px; line-height: 0; position: relative; vertical-align: baseline; top: -0.5em; color: rgba(0, 0, 0, 0.87); font-family: 'Noto Sans', -apple-system, BlinkMacSystemFont, 'Segoe UI', Roboto, Oxygen-Sans, Ubuntu, Cantarell, 'Helvetica Neue', sans-serif;">0</span><span style="color: rgba(0, 0, 0, 0.87); font-family: 'Noto Sans', -apple-system, BlinkMacSystemFont, 'Segoe UI', Roboto, Oxygen-Sans, Ubuntu, Cantarell, 'Helvetica Neue', sans-serif;"> and m, as presumed criteria of lipophilicity of examined cyanoacetamides were correlated by linear regression analysis with standard measure of lipophilicity, log P, with important pharmacokinetic predictors and selected parameters of toxicity. The established linear dependences are described by high regression coefficient values, r, which showed that RP TLC18 F</span><span style="font-size: 10.5px; line-height: 0; position: relative; vertical-align: baseline; bottom: -0.25em; color: rgba(0, 0, 0, 0.87); font-family: 'Noto Sans', -apple-system, BlinkMacSystemFont, 'Segoe UI', Roboto, Oxygen-Sans, Ubuntu, Cantarell, 'Helvetica Neue', sans-serif;">254s</span><span style="color: rgba(0, 0, 0, 0.87); font-family: 'Noto Sans', -apple-system, BlinkMacSystemFont, 'Segoe UI', Roboto, Oxygen-Sans, Ubuntu, Cantarell, 'Helvetica Neue', sans-serif;"> allows reliable determination of the lipophilicity of cyanoacetamides as potentially bioactive compounds.</span></p>

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