Thirty-four thiosemicarbazones and S-alkyl thiosemicarbazones, and some of their Zn(II) and Pd(II) complexes were obtained and purified to investigate antimicrobial activity. MIC values of the compounds were determined by the disc diffusion method against Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Salmonella typhi, Shigella flexneri, Staphylococcus aureus, S. epidermidis, and Candida albicans. The thiosemicarbazones show antibacterial and antifungal effects in free ligand and metal-complex form. Picolinaldehyde-S-methyl- and -S-benzylthiosemicarbazones did not affect the tested microorganisms but their Zn(II) complexes showed selective activity. The antimicrobial activity is relatively high in Me2SO, but the antimicrobial potential is changed in a certain range with Me2SO, HCONMe2, EtOH and CHCl3.
Antimicrobial activity of 2-(2-hydroxyphenyl)-5-R5-1H-benzimidazoles, 2-(2-hydroxy-5-R5'-phenyl)-1H-benzimidazoles and their FeIII, CuII, AgI, ZnII and HgII nitrate complexes was tested toward Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Salmonella typhi, Shigella flexneri, and Proteus mirabilis. Antifungal activity was tested against Candida albicans. Benzimidazole benzene ring substituents increase the antimicrobial activity, phenol ring substituents decrease it. The ligands show an antibacterial effect against only S. aureus whereas AgI and HgII complexes of the ligands have a higher activity with respect to the other complexes to all the bacteria. On the other hand, FeIII complexes show a considerable activity against S. aureus and S. epidermidis.
In the light of these findings, 5-chloro-1H-indole-2,3-dione 3-thiosemicarbazone derivatives were synthesized in order to obtain more potent and less toxic compounds. The structures of the ABSTRACT: A series of 5-chloro-1H-indole-2,3-dione 3-thiosemicarbazones 3a-g were synthesized to investigate the chemotherapeutic activities. The structures of 3a-g were confirmed by the spectral data (IR, 1 H NMR, 13 C NMR-APT, 13 C NMR-DEPT, HSQC, HMBC) and elemental analysis. Anticancer activities of the compounds were evaluated using cell kinetic parameters on HeLa cells derived from human cervix carcinoma. The preliminary screening results indicated that alkyl substituted compounds 3a, 3b and 3d were more effective in mitosis phase when compared to the synthesis phase. 3a-g were tested against some DNA and RNA viruses in CRFK, HeLa, HEL, MDCK and Vero cells. None of the compounds was active against any of the RNA or DNA viruses at 100 μM. All compounds were also evaluated for antimicrobial activity against selected strains. Methyl substituted 3a and allyl substituted 3c were found to be active against S. aureus and C. albicans.
2-(2-Pyridinyl)- (LI), 2-(6-methyl-2-pyridinyl)- (LII), 2-(6-methyl-2-pyridinyl)-5-methyl-(LIII), 2-(3-pyridinyl)- (LIV), 2-(3-pyridinyl)-5-methyl-1H-benzimidazoles (LV) and their complexes with Fe(NO3)3, Cu(NO3)2, Zn(NO3)2, and AgNO3 were synthesized and antibacterial activity of the compounds was tested toward Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Salmonella typhi, Shigella flexneri, Proteus mirabilis and antifungal activity against Candida albicans. The methyl groups of LIII increase the antimicrobial activity. The AgI complexes have considerable activity toward the microorganisms. Some ZnII complexes show an antimicrobial effect against S. aureus and S. flexneri, although the ligands themselves have no effect. CuII complexes have a considerable antibacterial effect to S. aureus and S. epidermidis.
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