ABSTRACT
1,3-Bis(2-benzimidazyl)-2-thiapropane(L) forms 5-coordinate square pyramidal and 4-coordinate tetrahedral, monometallic complexes with PdCl(2) and ZnX(2) (X=Cl, Br, I), respectively. In the palladium complex, the ligand acts as a chelating tridentate, through two of the nitrogen atoms in the imidazole ring and the sulfur atom of the bridging group together with two chloride ions forming a rare five coordinate complex. In the zinc halide complexes, the ligand acts as chelating bidentate, via two of the nitrogen atoms combined with two halide ions giving common tetrahedral complexes. The ligand and its complexes are characterized by analytical data and spectroscopic methods such as FT-Raman, FT-IR (mid-IR, far-IR), (1)H and (13)C NMR. Their antimicrobial activities are evaluated by the minimal inhibitory concentration (MIC) against 10 bacteria, each with multiple, fresh clinical isolates (10-15), and the results are compared with those of ampicillin, ciprofloxacin, cefazolin, ofloxacin, and piperacillin antibacterial agents. The compound's antifungal activities are reported on Candida albicans, Candida utilis, and Cryptococcus neoformans yeasts, each with multiple isolates (10), and the results are referenced with amphotericin-B, fluconazole and flucytosine antifungal agents. In most cases, the compounds show broad-spectrum (Gram(+) and Gram(-)) activities that are either, more active, or equipotent to, the antibiotic and antifungal agents in the comparison tests.
Subject(s)
Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Benzimidazoles/chemistry , Ligands , Palladium/chemistry , Propane/analogs & derivatives , Zinc/chemistry , Anti-Bacterial Agents/chemistry , Antifungal Agents/chemistry , Benzimidazoles/pharmacology , Chelating Agents/chemistry , Chelating Agents/pharmacology , Microbial Sensitivity Tests , Molecular Structure , Palladium/pharmacology , Propane/chemistry , Propane/pharmacology , Structure-Activity RelationshipABSTRACT
The 1,2-bis(2-benzimidazyl)-1,2-ethanediol (1), 1,4-bis(2-benzimidazyl)-1,2,3,4-butanetetraol (2), 1,3-bis(2-benzimidazyl)-2-thiapropane (3), 1,3-bis(2-benzimidazyl)-2-thia-propane-dihydrochloride (4), 1,5-bis(2-benzimidazyl)-3-thiapentane (5), and 1,5-bis(2-benzimidazyl)-3-thiapentane dihydrochloride (6) chelating ligands are synthesised and characterised by using analytical data and modem spectroscopic methods such as FT-Raman, FT-IR, 1H- and 13C-NMR spectrometers. Their antimicrobial activities are reported by comparing the in vitro activities, with those of ofloxacin, ciprofloxacin, piperacillin, ampicillin and cefazolin antibacterial agents against fresh clinical isolates. Antifungal activities are reported on Candida albicans, Candida utilis, Cryptococcus neoformans fungi, and the results are referenced with amphotericin-B, fluconazole and flucytosine antifungal agents. It has been found that all the compounds have broad spectra activity and was either more active or equipotent to those compared antibiotic and antifungal agents.