Events The 4th International Electronic Conference on Antibiotics

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Published

This submission belongs to the session S4. Novel Antimicrobial Agents: Discovery, Design, Synthesis and Action of the event The 4th International Electronic Conference on Antibiotics

Published date

19 May, 2025

Academic Editor

Jordi Vila

Citation

RAHUL MAITRA, Preeti Rana, Deepanshi Saxena, Abdul Akhir, Manasa Vadakattu, Abdul Kalam, Swanand Joshi, Ramulu Parupalli, Vasundhra Bhandari, Yaddanapudi Venkata Madhavi, Arunava Dasgupta, Sidharth Chopra, Srinivas Nanduri, Development of Naphthalimidehydrazide Derivatives as Potent Antibacterial Agents Against Carbapenem-resistant A. baumannii, in Proceedings of The 4th International Electronic Conference on Antibiotics, 21 May–23 May 2025, MDPI: Basel, Switzerland

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Development of Naphthalimidehydrazide Derivatives as Potent Antibacterial Agents Against Carbapenem-resistant A. baumannii

Preeti Rana ¹

RAHUL MAITRA ²

Deepanshi Saxena ²

Abdul Akhir ²

Manasa Vadakattu ¹

Abdul Kalam ¹

Swanand Joshi ¹

Ramulu Parupalli ¹

Vasundhra Bhandari ¹

Yaddanapudi Venkata Madhavi ¹

Arunava Dasgupta ²

Sidharth Chopra ²

Srinivas Nanduri ¹

1. Department of Chemical Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, India, India

2. Division of Molecular Microbiology and Immunology, CSIR-Central Drug Research Institute, Lucknow, India, India

Abstract

As per the WHO’s “Bacterial Priority Pathogen List”, Carbapenem-resistant A. baumannii (CRAB) is categorized as belonging to the critical priority pathogen group due to the extreme paucity of treatment options (1). A. baumannii causes several nosocomial infections such as pneumonia, sepsis and bacteraemia; skin and soft tissue infections; and meningitis (2). To respond to the urgent and unmet need of identifying novel antibiotics that are active against CRAB, we designed, synthesized and tested 29 naphthalimide derivatives by incorporating the hydrazine group against CRAB BAA-1605. From these compounds, 5b, 5c, 5d and 5e exhibited MICs ranging between 0.5 and 1 μg/ml, and all compounds except 5e displayed >200 selectivity indeces (SIs) against Vero cells. Compound 5d was chosen as a representative and tested against an MDR clinical strain panel, with strains that are resistant to meropenem, levofloxacin and minocycline. In these tests, 5d displayed equi-potent activity. In addition, 5d demonstrated synergy with tobramycin, and the synergy was confirmed by means of a combination time kill assay against CRAB BAA-1605. From the above data, 5d exhibits promise as a potential antibacterial scaffold against CRAB (3).

References:

https://iris.who.int/bitstream/handle/10665/376776/9789240093461-eng.pdf?sequence=1
Sieniawski, K., Kaczka, K., Rucinska, M., Gagis, L., & Pomorski, L. (2013). Acinetobacter baumannii nosocomial infections. Polski Przeglad Chirurgiczny/ Polish Journal of Surgery, 85(9), 483–490. https://doi.org/10.2478/pjs-2013-0075
https://doi.org/10.1039/D4MD00368C

Keywords

CRAB

Bacteraemia,

Synthesis and Antibacterial Action of New Ni(II), Pd(II) and Pt(II) Complexes with Benzimidazole-Derived Schiff Base Ligands

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