SYNTHESIS AND BIOLOGICAL EVALUATION OF THE PROGENITOR OF A NEW CLASS OF CEPHALOSPORIN ANALOGUES, WITH A PARTICULAR FOCUS ON STRUCTURE-BASED COMPUTATIONAL ANALYSIS.

Synthesis and biological evaluation of the progenitor of a new class of cephalosporin analogues, with a particular focus on structure-based computational analysis.

Synthesis and biological evaluation of the progenitor of a new class of cephalosporin analogues, with a particular focus on structure-based computational analysis.

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We present the synthesis and biological evaluation of the prototype of a new class of cephalosporins, containing an additional isolated beta lactam ring with two phenyl substituents.This new compound is effective against Gram positive microorganisms, with a potency similar to 8n joico lumishine that of ceftriaxone, a cephalosporin widely used in clinics and taken as a reference, and with no cytotoxicity against two different human cell lines, even at a concentration much higher than the minimal inhibitory concentration tested.Additionally, a deep computational analysis has been conducted with the cap sleeve layering tee aim of understanding the contribution of its moieties to the binding energy towards several penicillin-binding proteins from both Gram positive and Gram negative bacteria.All these results will help us developing derivatives of this compound with improved chemical and biological properties, such as a broader spectrum of action and/or an increased affinity towards their molecular targets.

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