抗细菌水杨酸酯的杂环同分异构体

Josef Matyk , Karel Waisser , Kateřina Dražková , Jiří Kuneš , Věra Klimešová , Karel Palát Jr. , Jarmila Kaustová
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引用次数: 19

摘要

合成了一系列64个水杨酸苯胺取代杂环类似物衍生物。测定了化合物对结核分枝杆菌、鸟分枝杆菌和两株堪萨斯分枝杆菌的体外抑菌活性。对于QSAR研究,采用Free-Wilson方法与Hansch方法相结合的方法。在杂环和水杨基上分离了分子,并研究了电子和疏水性对分子的影响。这些化合物是一类潜在的新型抗结核药物。
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Heterocyclic isosters of antimycobacterial salicylanilides

A series of 64 derivatives of substituted heterocyclic analogues of salicylanilides was synthesized. The compounds were evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium avium and two strains of Mycobacterium kansasii. For the QSAR study, the combination of Free–Wilson approach with Hansch approach was used. The molecules were separated on the heterocyclic and salicyl moieties and the study of influences of electronic and hydrophobic properties was used as well. The compounds are a new group of potential antituberculotics.

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