Bacterial infections, caused predominately by Gram-positive and Gram-negative organisms, are proliferation of harmful strains of bacteria on or inside the body. Hospital-acquired and community-acquired bacterial infections have already put a heavy burden on the global health system. Antibiotics can disrupt the processes necessary for bacterial cell growth and proliferation, are effective weapons to fight against bacterial infections. However, the overuse and misuse of antibiotics have led to a rise in antibiotic resistance, creating an urgent need to develop novel antibiotics. 1,2,4-Triazole-quinoline/quinolone hybrids possess a broad spectrum of chemotherapeutic properties, also demonstrated promising anti-bacterial activities against both drug-sensitive and drug-resistant bacteria. This review covers the recent advances of 1,2,4-triazole-quinoline/quinolone hybrids as potential anti-bacterial agents. The structure-activity relationship (SAR) is also discussed for further rational development of 1,2,4-triazole hybrids higher potency against both drug-sensitive and drug-resistant pathogens.