Synthesis and QSAR Studies of Claramine Derivatives, a New Class of Broad-Spectrum Antimicrobial Agents

The development of new antibiotics has been recognized for over two decades as a major challenge in combating multidrug-resistant bacteria. Herein, we report the synthesis and QSAR studies of claramine derivatives, a new class of broad-spectrum antimicrobial agents active against both susceptible and resistant Gram-positive and Gram-negative strains. The observed antimicrobial activities were rationalized based on key topological parameters of the derivatives, while cytotoxicity was interpreted by correlating half maximal inhibitory concentration (IC<sub>50</sub>) values with QSAR models. Owing to the low cytotoxicity observed for several analogues, this molecular class represents a promising alternative for the development of novel agents to counteract multidrug resistance.

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Publication Details

Journal
Molecules
Published
2025-12-01
DOI
https://doi.org/10.3390/molecules30234614
Primary Topic
Antimicrobial agents and applications
Type
article
Field-Weighted Citation Impact
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article

Synthesis and QSAR Studies of Claramine Derivatives, a New Class of Broad-Spectrum Antimicrobial Agents

Jean Michel Brunel, Carole Di Giorgio, Marine Blanchet
Molecules
Antimicrobial agents and applications
article

Synthesis and QSAR Studies of Claramine Derivatives, a New Class of Broad-Spectrum Antimicrobial Agents

Jean Michel Brunel, Carole Di Giorgio, Marine Blanchet
article en

Abstract

The development of new antibiotics has been recognized for over two decades as a major challenge in combating multidrug-resistant bacteria. Herein, we report the synthesis and QSAR studies of claramine derivatives, a new class of broad-spectrum antimicrobial agents active against both susceptible and resistant Gram-positive and Gram-negative strains. The observed antimicrobial activities were rationalized based on key topological parameters of the derivatives, while cytotoxicity was interpreted by correlating half maximal inhibitory concentration (IC<sub>50</sub>) values with QSAR models. Owing to the low cytotoxicity observed for several analogues, this molecular class represents a promising alternative for the development of novel agents to counteract multidrug resistance.

MoleculesVol. 30(23)
Centre National de la Recherche Scientifique (FR), Inserm (FR), Aix-Marseille Université (FR), Institut de Recherche pour le Développement (FR)
Openalex Percentile: Top 71%
Antimicrobial agents and applications
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