Pyrrole-thiazolidinone hybrids as a new structural class of broad-spectrum anti-infectives

被引：6
作者：
Ahmed, Shujauddin [1 ]
Mital, Alka [1 ]
Akhir, Abdul [2 ]
Saxena, Deepanshi [2 ]
Ahmad, Mohammad Naiyaz [2 ]
Dasgupta, Arunava [2 ,3 ]
Chopra, Sidharth [2 ,3 ]
Jain, Rahul [1 ]
机构：
[1] Natl Inst Pharmaceut Educ & Res, Dept Med Chem, Sect 67, SAS Nagar 160062, Punjab, India
[2] Cent Drug Res Inst CSIR CDRI, Div Mol Microbiol & Immunol, Sect 10,Jankipuram Extens,Sitapur Rd, Lucknow 226031, Uttar Pradesh, India
[3] Acad Sci & Innovat Res AcSIR, Ghaziabad 201002, India
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2023年 / 260卷
关键词：
Antimicrobial; Anti-TB; ESKAP bacteria; Thiazolidinone; Pyrrole; ANTIMICROBIAL ACTIVITY; BIOLOGICAL EVALUATION; POTENTIAL ANTICANCER; DERIVATIVES; PYRROLNITRIN; DISCOVERY; DESIGN; AGENTS; IMIDAZO<4,5-C>PYRIDINES; 4-THIAZOLIDINONES;
D O I：
10.1016/j.ejmech.2023.115757
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of pyrrole-thiazolidinone hybrids was designed, synthesized and evaluated for activities against ESKAP bacteria panel and mycobacterial pathogens. From the series, compound 9d showed prominent activity against S. aureus (MIC = 0.5 mu g/mL) and compound 9k showed the most promising activity against M. tuberculosis H37Rv (MIC = 0.5 mu g/mL). Potent derivatives were found to be non-toxic when tested against Vero cells. Compound 9d upon evaluation in vitro against several MRSA and VRSA strains produced activity comparable or better than standard drugs. In the anti-biofilm assay, 9d reduced S. aureus biofilm by >11% at 10x MIC. The dual inhibitory effect exhibited by pyrrole-thiazolidinone hybrids confirms their potential as new class of promising antiinfective agents.
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页数：13
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