Work

Design, Synthesis, and Activity Evaluation of Novel Bifenamide Dual-Target Antibacterial Inhibitors and Carrier Based on Infectious Microenvironment

Year: 2025

Type: article

Abstract: As the external environment worsens and immune function declines, Gram-negative bacterial infections are causing more and more serious pathological damage. In the study, three series of novel bifenamide dual-target (PD-L1/LpxC) compounds were designed using the skeleton growth method. Their chemical structures were synthesized, characterized, and evaluated for antibacterial activity. Among them, the compound 12b, which exhibited excellent dual-target (PD-L1/LpxC) inhibition ability, could efficiently block the biosynthesis of bacterial lipopolysaccharide (LPS), leading to pathogenic cell lysis and death. Moreover, the nanocomposite (NC- 12b ) was also prepared based on the infection microenvironment to improve the bioavailability and targeting of compound 12b . In vivo evaluation confirmed the dual functions of these components, including bacterial inhibition and immune activation, thereby synergistically accelerating the body’s recovery process.

Source: Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.4c02913

Authors: Shuai Yu, Shiying Zhang, Anli Zhang, Jun Han, Bin Sun

Institution: Liaocheng University

Language: English

Topic: Synthesis and Biological Evaluation

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: green

Funders: National Natural Science Foundation of China, Liaocheng University, Natural Science Foundation of Shandong Province