Synthesis of sulbactam derivatives shows improved antibacterial activity against Acinetobacter baumannii, indicating potential for oral medication.
Sulbactam, a known β-lactamase inhibitor, was found to own potent antimicrobial activity against Acinetobacter baumannii in clinical practice. Based on clinical evidence, a series of sulbactam derivatives were designed, synthesized and evaluated for antibacterial activity against Acinetobacter baumannii, taking sulbactam as the lead. Among them, compound 9 exhibited a good antibacterial activity against Acinetobacter baumannii with a MIC value of 4 μg/mL, slightly lower than that of sulbactam of 1 μg/mL. Especially, compound 9 displayed outstanding oral pharmacokinetic profiles with a maximum plasma concentration (Cmax) of 19.6 μg/mL and area under the curve (AUC) of 10.8 μgh/mL, much higher than those of sulbactam, and thus held the potential of being developed into an oral medication. These results provided the useful information for further structural modification and optimization of its kind, and compound 9 has been selected for the further investigation.
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Yang et al. (2018) studied this question.
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