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EFFICIENT SYNTHESIS OF DHA TRANSITION METAL CHELATES AS POTENT ANTIOXIDANTS, ENZYME INHIBITOR AND ANTIMICROBIAL AGENTS.
* 1 , 2 , 1 , 3 , 1
1  Université frères Mentouri-Constantine 1, Laboratoire d'Obtention de Substances Thérapeutiques (LOST), Campus Chasbet Ersas, 25000 Constantine, Algérie.
2  Université frères Mentouri-Constantine 1, Laboratoire Physicochimie Analytique et Cristallochimie de Matériaux Organométalliques et Biomoléculaires, Algérie.
3  Centre de Recherche en Biotechnologie CRBt, Constantine2, Algérie.

Abstract:

There is a growing interest on dehydroacetic acid DHA derivatives compounds in recent years, due to an establish antibacterial, antifungal, anti-inflammatory and anticancer activities. Several researches were performed on ligand precursor and transition metal complexes derivatives.

Efficient and easy access to a transition metal chelates series with acid DHA as starting materials is reported, the obtained compounds were fully characterized by MP, UV-Vis and FT-IR spectroscopy, several in vitro biological tests were also performed on obtained metal chelates to explore its therapeutically potential in order to continue further investigations and exploring it as new target drugs. In this case, enzymatic activity: as urease inhibitors and antioxidant activities: ABTS free radical scavenging activity, β-carotène linoleic acid bleaching activity, Ferrous ions binding effect, Copper and ferrous chelating activity, gave good values of IC50 for all studied complexes 1-4 in range of 8,20 ±0,39-10,62 ±0,01 μg/mL for urease inhibiting test better than DHA and used standard Thiourea (IC50=11,57±0,68 μg/mL), interesting results are also obtained for compound 2 in ability of chelating ferrous ions with an IC50=14,53±0,92 μg/mL, comparing with tested standard EDTA (CI50=8,80±0,47 μg/mL), for all cited applications complex 4 is mostly a hit, while antimicrobial activity gave better results with free ligand DHA, discussion on molecular structure and predicted structure activity relationship will be given.

Keywords: DHA, Transition metal complexes, Biological activities.
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