The Strategies of Pathogen-Oriented Therapy on Circumventing Antimicrobial Resistance

Table 1

Examples of AACs.


Antibiotic conjugates		Evaluated condition	Proposed mechanism of action	Reference

Quinolone/fluoroquinolone	Quinolone-oxazolidinone (MCB3681)	Gram-positive bacterial infections	Inhibit the initiation of bacterial protein biosynthesis	[26, 27]
	Quinolizine-rifamycin (cadazolid)	C. difficile infections	Inhibit protein and RNA synthesis	[28–30]
	Fluoroquinolone-oxazolidinone (CBR-2092)	Gram-positive bacterial infections	Inhibit the bacterial DNA replication and DNA-dependent RNA synthesis	[31, 32]

Aminoglycoside	Neomycin B-ciprofloxacin	Gram-negative bacteria and Gram-positive MRSA infections	Inhibit the activity of DNA gyrase, topoisomerase IV, and protein synthesis	[33]
	Tobramycin-moxifloxacin	Pseudomonas aeruginosa infections	Enhance the permeability of antibiotics to the outer membrane of pathogenic bacteria	[34, 35]
	Neomycin-sisomicin	Aminoglycoside-resistant bacteria infections	Inhibit protein synthesis by binding to 16S rRNA	[36, 37]

β-Lactamase inhibitor	Ceftazidime-avibactam	Complicated urinary tract infections	Interfere with bacterial cell wall and peptidoglycan synthesis	[22, 38]
	Meropenem-vaborbactam	Complicated urinary tract infections and acute pyelonephritis	Vaborbactam potentiates the activity of meropenem, inhibiting the cell wall synthesis and peptidoglycan synthesis	[20, 39, 40]
	Imipenem-relebactam	Gram-negative bacterial infections	Relebactam prevents the hydrolysis of imipenem, exerting imipenem’s bactericidal effect	[41, 42]

Macrolide	Azithromycin-sulfonamide	Macrolide-resistant Streptococcus pyogenes and Streptococcus pneumoniae strains	Inhibit mRNA translation and bacterial metabolic processes	[43, 44]