5440-97-1Relevant academic research and scientific papers
Preparation and characterization of sulfadiazine Schiff base complexes of Co(II), Ni(II), Cu(II), and Mn(II)
El-Baradie, Kamal Y.
, p. 1139 - 1155 (2005)
Complexes of Co(II), Ni(II), Cu(II), and Mn(II) containing Schiff base NOS donor ligands have been synthesised via chemical and electrochemical techniques. The structure of the complexes has been elucidated by elemental analysis, conductance, magnetic sus
Sulfadiazine salicylaldehyde-based schiff bases: Synthesis, antimicrobial activity and cytotoxicity
Krátky, Martin,Dzurková, Magdaléna,Janou?ek, Ji?í,Kone?ná, Klára,Trejtnar, Franti?ek,Stola?íková, Ji?ina,Vin?ová, Jarmila
, (2017/09/25)
The resistance among microbes has brought an urgent need for new drugs. Thus, we synthesized a series of Schiff bases derived from the sulfa drug sulfadiazine and various salicylaldehydes. The resulting 4-[(2-hydroxybenzylidene)amino]-N-(pyrimidin-2-yl)benzene-sulfonamides were characterized and evaluated against Gram-positive and Gram-negative bacteria, yeasts, moulds, Mycobacterium tuberculosis, nontuberculous mycobacteria (M. kansasii, M. avium) and their cytotoxicity was determined. Among bacteria, the genus Staphylococcus, including methicillin-resistant S. aureus, showed the highest susceptibility, with minimum inhibitory concentration values from 7.81 μM. The growth of Candida sp. and Trichophyton interdigitale was inhibited at concentrations starting from 1.95 μM. 4-[(2,5-Dihydroxybenzylidene)amino]-N-(pyrimidin-2-yl)-benzenesulfonamide was identified as the most selective Schiff base for these strains with no apparent cytotoxicity and a selectivity index higher than 16. With respect to M. tuberculosis and M. kansasii that were inhibited within the range of 8 to 250 μM, unsubstituted 4-[(2-hydroxy-benzylidene)amino]-N-(pyrimidin-2-yl)benzenesulfonamide meets the selectivity requirement. In general, dihalogenation of the salicylic moiety improved the antibacterial and antifungal activity but also increased the cytotoxicity, especially with an increasing atomic mass. Some derivatives offer more advantageous properties than the parent sulfadiazine, thus constituting promising hits for further antimicrobial drug development.
