List of antibacterial drugs

S. No.StructureDrugMechanism of actionMechanism of resistanceReferences
1TedizolidBinds to 23S rRNA in the 50S ribosomal subunit, blocking protein synthesis initiation and aminoacyl-tRNA binding in bacteria.Resistance arises through 23S rRNA mutations or cfr gene transfer, reducing the drug’s ribosomal binding affinity.[96]
2Ceftolozane-tazobactamCombines bactericidal effects of ceftolozane with tazobactam’s β-lactamase inhibition.Resistance involves metallo-β-lactamases and AmpC hyperproduction, reducing drug efficacy.[97]
3OritavancinInhibits peptidoglycan synthesis by binding to D-Ala-D-Ala and D-Ala-D-Lac, blocking transglycosylation and transpeptidation.Resistance due to changes in VanB operon expression or D-Lac precursor presence, which reduce drug sensitivity.[98]
4Ceftazidime-AvibactamCeftazidime disrupts cell wall synthesis via penicillin-binding proteins (PBPs); avibactam inhibits ceftazidime breakdown by β-lactamases.Resistance stems from metallo-β-lactamases, specific class D enzymes, mutations in β-lactamase enzymes (e.g., KPC-3), along with reduced permeability and efflux.[99]
5MeropenemInhibits cell wall synthesis by binding to PBPs; vaborbactam enhances efficacy by inhibiting class A β-lactamases.Resistance mechanisms include class B and D carbapenemases, altered PBPs, and increased efflux pump activity.[100]
6PretomanidIn anaerobic conditions, generates reactive intermediates that inhibit respiration in non-replicating bacteria and disrupt protein and lipid synthesis in replicating bacteria.Resistance primarily occurs through mutations in activation-related genes (e.g., Ddn, Fgd, fbiA/B/C), sometimes affecting CofC or rplC and conferring dual resistance with linezolid.[101]
7LefamulinBinds to the 50S ribosomal subunit, inhibiting peptide bond formation and protein synthesis in bacteria.Resistance arises from genes like vga(A), cfr, and mutations in 23S rRNA and ribosomal proteins (rplC, rplD).[102]
8SarecyclineBinds to the bacterial ribosome’s A site, blocking mRNA translation; also reduces inflammation by suppressing cytokines and neutrophil activation.Resistance occurs through degradation, rRNA mutations, ribosomal protection (e.g., TetM, TetO), and efflux pumps like TetA.[103]
9PlazomicinInhibits protein synthesis by binding to the A-site of 16S rRNA in the 30S ribosomal subunit in Gram-negative bacteria.
Resistance is mostly due to aminoglycoside-modifying enzymes (AMEs), target site alterations, and changes in porin or efflux pump expression.[104]
10HalicinExhibits broad-spectrum antibacterial action by damaging DNA and disrupting the proton motive force (PMF), impeding bacterial adaptation and resistance.Resistance is rare and mainly involves mutations affecting protein synthesis, transport, and nitroreduction.[105]
11ZoliflodacinInhibits bacterial type 2 topoisomerase, primarily targeting DNA gyrase, preventing fluoroquinolone cross-resistance and double-strand DNA breaks.Resistance is uncommon, associated with gyrB gene alterations, and presents minimal cross-resistance with other antibiotics.[106]
12DurlobactamRestores Acinetobacter baumannii’s susceptibility to sulbactam by inhibiting class D carbapenemases, β-lactamases, and reducing PBP2.Resistance may occur through metallo-β-lactamases, certain PBP mutations, and the AdeIJK efflux system.[107]
13OpelconazoleInhibits 14-α-demethylase (CYP51A), blocking ergosterol formation in fungal cell membranes, effective against Aspergillus and Mucorales.Resistance primarily arises from ERG11 gene mutations, notably TR34/L98H in cyp51A, which reduce drug binding efficacy.[108]