Development of naphthalimide hydrazide derivatives as potent antibacterial agents against carbapenem-resistant A. baumanniiElectronic supplementary information (ESI) available. See DOI: https://doi.org/10.1039/d4md00368c

Autor: Rana, Preeti, Maitra, Rahul, Saxena, Deepanshi, Akhir, Abdul, Vadakattu, Manasa, Kalam, Abdul, Joshi, Swanand Vinayak, Parupalli, Ramulu, Bhandari, Vasundhra, Madhavi, Y. V., Dasgupta, Arunava, Chopra, Sidharth, Nanduri, Srinivas
Zdroj: MedChemComm; 2024, Vol. 15 Issue: 12 p4011-4017, 7p
Abstrakt: In this work, a novel series of naphthalimide hydrazide derivatives were designed, synthesized and evaluated against a bacterial pathogen panel. Most of the compounds were found to exhibit potent antibacterial activity against carbapenem-resistant A. baumanniiBAA 1605, with MIC ranging from 0.5 to 16 μg mL−1. Compounds 5b, 5c, 5dand 5eshowed the most potent antibacterial activity, with an MIC range of 0.5–1 μg mL−1. These compounds were also found to be non-toxic to Vero cells with a high selectivity index. Further, they were active against 24 clinical isolates of MDR-AB with potent antibacterial activity. In addition, synergistic studies revealed that compound 5dexhibited synergism with FDA-approved drugs, as further validated through time-kill kinetic studies. These results highlight the potential of the synthesized compounds as promising leads for the development of novel and selective agents against carbapenem-resistant A. baumannii.
Databáze: Supplemental Index