Parasitic diseases symbolize major world health problem with limited therapeutic options, most of the available treatments being decades old and suffering from limited efficiency and/or undesirable side effects. In search for a pharmacological control of these tropical diseases, such as trypanosomiasis, an introduction of a Lewis acid, metal ions, into the available organic drug through metal-drug synergism phenomenon has recently provided a promising way out. The use of metal complexes as chemotherapeutic agents against these ailments appears a very attractive alternative. This study was aimed at synthesizing and characterizing some novel transition metal complexes of 2,5-diamino-2(difluoromethyl)pentanoic acid Hydrochloride-1- Hydrate (DPH). Antibacterial screening and toxicological studies on some selected metal complexes were also achieved. The metal complexes were synthesized using standard methods with slight modifications and were obtained with appreciably good yield. The complexes were characterized by techniques like melting point, elemental analysis, UV-Vis., conductivity measurements, FTIR, ESI-MS, magnetic susceptibility measurement and X-ray crystallography. The in-vitro antibacterial efficacies of metal complexes were examined using some medically important bacterial isolates. The in-vivo toxicological screening was investigated using albino rats. The spectroscopic techniques data revealed that DPH acted as a bidentate ligand and metal complexes are new and possess zwitterionic structures. X-ray crystal structure of [Cu(DPH)Cl2]·H2O obtained represents the first Cu(II) crystal structure of DPH with M-X-M-X infinite chain structure. The metal-drug complexes exhibited lethal effect against the test organisms than DPH and antibacterial potency appeared to be concentration dependent as degree of inhibition increases with increase in concentration. The outcome of this study generally indicated that new potent compounds with better properties and enhanced antibacterial activities upon complexation have been synthesized. Spectral data and X-ray crystallography ascertained the composition, structure and mode of coordination of metal-ligand chelates. Detailed syntheses, characterisation, physicochemical properties and biological potency of these chelates as highlighted above will be discussed.

Novel transition metal(II)-2,5-diamino-2(difluoromethyl)pentanoic acid hydrochloride-1- hydrate complexes: Syntheses, characterization, structural elucidation, and their biological potency

249th National Meeting (2015)

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