Synthesis and biological evaluation of sulfonamide thiazole and benzothiazole derivatives as antimicrobial agents

被引:110
|
作者
Argyropoulou, Iro [1 ]
Geronikaki, Athina [1 ]
Vicini, Paola [2 ]
Zani, Franca [2 ]
机构
[1] Aristotle Univ Thessaloniki, Sch Pharm, Dept Pharmaceut Chem, GR-54006 Thessaloniki, Greece
[2] Univ Parma, Dipartimento Farmaceut, I-43100 Parma, Italy
关键词
Thiazole derivatives; benzothiazole derivatives; sulfonamides; antimicrobial activity; CARBONIC-ANHYDRASE INHIBITORS; LOCAL-ANESTHETIC ACTIVITY;
D O I
10.3998/ark.5550190.0010.611
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Several thiazoles and benzothiazoles carrying a benzenesulfonamide moiety at position 2 of the heterocyclic nucleus were synthesised and tested as antimicrobial agents. All sulfanilamides and some of the nitro substituted sulfonamides have effective antibacterial properties against Gram positive bacteria (MIC 0.3-100 mu g/mL) such as several bacilli, staphylococci and streptococci, including methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis strains. On the contrary, no inhibition of Gram negative Escherichia coli and fungi is detected up to the concentration of 100 mu g/mL. Synergistic inhibitory activity occurs when the active antibacterial sulfonamides are tested in combination with trimethoprim against both Bacillus subtilis and Staphylococcus aureus.
引用
收藏
页码:89 / 102
页数:14
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