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Magorzata Szczesio Andrzej Olczak Katarzyna Gobis Ida Mazerant Sylwia Kauyska Henryk Foks Marek L. Gwka 《Acta Crystallographica. Section C, Structural Chemistry》2016,72(1):75-79
The emergence of drug‐resistant strains of Mycobacterium tuberculosis has intensified efforts to identify new lead tuberculostatics. Our earlier studies concluded that the planarity of a molecule correlates well with its tuberculostatic activity. According to our hypothesis, only derivatives whose molecules are capable of adopting a planar conformation may show tuberculostatic activity. The structures of three new potentially tuberculostatic compounds, namely N′‐[bis(methylsulfanyl)methylidene]‐N‐methyl‐4‐nitrobenzohydrazide (denoted G1), C11H13N3O3S2, N′‐[bis(benzylsulfanyl)methylidene]‐N‐methyl‐4‐nitrobenzohydrazide (denoted G2), C23H21N3O3S2, and N′‐[(benzylsulfanyl)(methylsulfanyl)methylidene]‐4‐nitrobenzohydrazide (denoted G3), C16H15N3O3S2, were determined by X‐ray diffraction. The significant distortion from planarity caused by the methyl substituent at the N atom of the hydrazide group or the NO2 substituent in the aromatic ring leads to the loss of tuberculostatic activity for G1, G2 and G4 {systematic name: N′‐[bis(methylsulfanyl)methylidene]‐2‐nitrobenzohydrazide}. A similar effect is observed when there are large substituents at the S atoms (G2 and G3). 相似文献
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《Acta Crystallographica. Section C, Structural Chemistry》2017,73(2):84-90
Searches for new tuberculostatic agents are important considering the occurrence of drug‐resistant strains of Mycobacterium tuberculosis . The structures of three new potentially tuberculostatic compounds, namely isopropyl methyl (2‐hydroxybenzoyl)carbonohydrazonodithioate, C12H16N2O2S2, (Z )‐benzyl methyl (2‐hydroxybenzoyl)carbonohydrazonodithioate, C16H16N2O2S2, and dibenzyl (2‐hydroxybenzoyl)carbonohydrazonodithioate propan‐2‐ol monosolvate, C22H20N2O2S2·C3H8O, were determined by X‐ray diffraction. The mutual orientation of the three main fragments of the compounds, namely an aromatic ring, a dithioester group and a hydrazide group, can influence the biological activity of the compounds. In all three of the structures studied, the C(=O)NH group is in the anti conformation. In addition, the presence of the hydroxy group in the ortho position of the aromatic ring in all three structures leads to the formation of an intramolecular hydrogen bond stabilizing the planarity of the molecules. 相似文献
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