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High-performance liquid chromatography evaluation of lipophilicity and QSRR modeling of a series of dual DNA gyrase and topoisomerase IV inhibitors [Elektronski vir]Dobričić, Vladimir ...Bacterial DNA gyrase and topoisomerase IV control the topological state of DNA during replication and represent important antibacterial drug targets. To be successful as drug candidates, newly ... synthesized compounds must possess optimal lipophilicity, which enables efficient delivery to the site of action. In this study, retention behavior of twenty-three previously synthesized dual DNA gyrase and topoisomerase IV inhibitors was tested in RP-HPLC system, consisting of C8 column and acetonitrile/phosphate buffer (pH 5.5 and pH 7.4) mobile phase. logD was calculated at both pH values and the best correlation with logD was obtained for retention parameter φ0, indicating that this RP-HPLC system could be used as an alternative to the shake-flask determination of lipophilicity. Subsequent QSRR analysis revealed that intrinsic lipophilicity (logP) and molecular weight (bcutm13) have a positive, while solubility (bcutp3) has a negative influence on this retention parameter.Vrsta gradiva - e-članek ; neleposlovje za odrasleLeto - 2022Jezik - angleškiCOBISS.SI-ID - 132432387
Avtor
Dobričić, Vladimir |
Savić, Jelena, farmacevtka |
Tomašič, Tihomir |
Durcik, Martina |
Zidar, Nace |
Peterlin-Mašič, Lucija |
Ilaš, Janez |
Kikelj, Danijel |
Čudina, Olivera
Teme
Zdravila |
Tekočinska kromatografija |
protibakterijska zdravila |
zaviralci topoizomeraze IV |
bakterijska DNA giraza |
tekočinska kromatografija visoke ločljivosti
Vnos na polico
Trajna povezava
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Dobričić, Vladimir | |
Savić, Jelena, farmacevtka | |
Tomašič, Tihomir | 28334 |
Durcik, Martina | 50490 |
Zidar, Nace | 28905 |
Peterlin-Mašič, Lucija | 19317 |
Ilaš, Janez | 24400 |
Kikelj, Danijel | 01463 |
Čudina, Olivera |
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