Design, synthesis, and integrated biological and molecular modeling studies of ciprofloxacin–amino acid derivatives as multi-target antimicrobials

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Authors: Ahmed M. Kamal El-sagheir, Margareth Sidarta, Alex Bunker, Michaela Wenzel, Jari T. Yli‐Kauhaluoma
Cited by: 1
References: 62

Abstract

Fluoroquinolones are broad-spectrum antibacterials that exert their effects by inhibiting DNA gyrase and topoisomerase IV, enzymes crucial for bacterial DNA replication. Here, we report the synthesis of 60 novel ciprofloxacin-amino acid derivatives, designed to inhibit multiple bacterial targets by the so-called polypharmacology approach. Some of the synthesized compounds retained or improved the antibacterial potency against Gram-positive, Gram-negative, and mycobacterial species. Notably, some derivatives demonstrated promising activity (MIC

Fields of Study & Subjects

Cancer therapeutics and mechanisms Antibiotics Pharmacokinetics and Efficacy Synthesis and biological activity

Publication details

Journal / source
European Journal of Medicinal Chemistry
Publisher
Elsevier BV
Volume
318
Pages
119138–119138
Publication date
9 July 2026
Language
EN