Abstract
Due to the rapidly growing bacterial resistance to antibiotics and the scarcity of novel agents under development, bacterial infections are still a pressing global problem, making new types of antibacterial agents, which are effective both alone and in combination with traditional antibiotics, urgently needed. In this paper, seven series of N-arylsulfonylindole analogs 5–11 bearing rhodanine moieties were synthesized, characterized, and evaluated for antibacterial activity. According to the in vitro antimicrobial results, half of the synthesized compounds showed potent inhibition against four Gram-positive bacteria, with MIC values in the range of 0.5–8 µg/mL. For multidrug-resistant strains, compounds 6a and 6c were the most potent, with MIC values of 0.5 µg/mL, having comparable activity to gatifloxacin, moxiflocaxin and norfloxacin and being 128-fold more potent than oxacillin (MIC = 64 µg/mL) and 64-fold more active than penicillin (MIC = 32 µg/mL) against Staphylococcus aureus ATCC 43300.
Highlights
Bacterial drug resistance has emerged and become increasingly serious on a global scale, both in developed and developing countries [1]
The development of new antimicrobial drugs cannot keep pace with the development of bacterial drug resistance, and the number of new antibiotics approved for marketing per year is declining continuously
Taking advantage of pathogens virulence is an alternative strategy to inhibit antibiotic resistance development, and some studies have focused on anti-virulence agents against Gram-positive pathogens and Gram-negative pathogens [7,8]
Summary
Bacterial drug resistance has emerged and become increasingly serious on a global scale, both in developed and developing countries [1]. Taking advantage of pathogens virulence is an alternative strategy to inhibit antibiotic resistance development, and some studies have focused on anti-virulence agents against Gram-positive pathogens and Gram-negative pathogens [7,8] This strategy has some weaknesses that limiting its development, such as the lack of a good way to assessing the efficacy and the inapplicability in immunocompromised patients. A few new antibiotics (e.g., linezolid, ceftolozane, telavancin, ceftaroline fosamil, Xifaxan®, and daptomycin) were approved and dozens of antibiotics are currently in Phase 2 or Phase 3 clinical trials [9] These drugs cannot address the entire spectrum of bacteria resistance [10], there is an urgent need to develop new antimicrobial agents, especially those with a new drug target or with the ability to overcome drug resistance
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