Abstract
We report herein three novel complexes whose design was based on the approach that consists of combining commercially available antibiotics with metals to attain different physicochemical properties and promote antimicrobial activity. Thus, new isostructural three-dimensional (3D) hydrogen bonding frameworks of pipemidic acid with manganese (II), zinc (II) and calcium (II) have been synthesised by mechanochemistry and are stable under shelf conditions. Notably, the antimicrobial activity of the compounds is maintained or even increased; in particular, the activity of the complexes is augmented against Escherichia coli, a representative of Gram-negative bacteria that have emerged as a major concern in drug resistance. Moreover, the synthesised compounds display similar general toxicity (Artemia salina model) levels to the original antibiotic, pipemidic acid. The increased antibacterial activity of the synthesised compounds, together with their appropriate toxicity levels, are promising outcomes.
Highlights
Quinolone antibiotics are broad-spectrum synthetic antibacterial compounds that exhibit, in most cases, appropriate oral absorption and bioavailability [1,2]
We present three isostructural hydrogen bonding frameworks built from pipemidic acid acid metal complexes successfully prepared by mechanochemistry [44,45,46], a privileged synthetic metal complexes successfully prepared by mechanochemistry [44,45,46], a privileged synthetic technique, in the solid state due to its reduced reaction times, lack or minimal usage of solvent, technique, in the solid state due to its reduced reaction times, lack or minimal usage of solvent, selectivity enhancement and novel reactivity [47,48]
We present three novel metal–coordination complexes of pipemidic acid with safe metals (Mn(II), Zn(II) and Ca(II)). These compounds were synthesised from liquid-assisted grinding (LAG). Mechanochemistry and their structural characterisation unveiled an isostructural character despite the different metal centres
Summary
Quinolone antibiotics are broad-spectrum synthetic antibacterial compounds that exhibit, in most cases, appropriate oral absorption and bioavailability [1,2]. This addition increased lipophilicity compound, aforementioned to [12,13]. Quinolone studied the antimicrobial activity ofsolubility several pipemidic acid compared to the free antibiotic [20,21]. Bearing all this in mind, the selected biocompatible metals for this study were calcium, manganese. Artemia salina salina [50,51]
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