November 2017 Convenient Synthesis and Biological Activity of Mono and Diacyl 2,5-Dimercapto-1,3,4-thiadiazole Derivatives

被引:2
|
作者
Jasiak, Karolina [1 ]
Kudelko, Agnieszka [1 ]
Wroblowska, Monika [1 ]
Biernasiuk, Anna [2 ]
Malm, Anna [2 ]
Krawczyk, Maria [3 ]
机构
[1] Silesian Tech Univ, Dept Chem Organ Technol & Petrochem, Krzywoustego 4, PL-44100 Gliwice, Poland
[2] Med Univ, Fac Pharm, Dept Pharmaceut Microbiol, Chodzki 1, PL-20093 Lublin, Poland
[3] Inst Ind Organ Chem, Annopol 6, PL-03236 Warsaw, Poland
关键词
ANTIMICROBIAL ACTIVITY; ANTIFUNGAL ACTIVITY; 1,3,4-THIADIAZOLES;
D O I
10.1002/jhet.2942
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
New derivatives of 2,5-dimercapto-1,3,4-thiadiazole substituted both at one or two exocyclic sulfur atoms with a series of aroyl or ethoxycarbonyl groups were synthesized in reactions of 2,5-dimercapto-1,3,4-thiadiazole salts with appropriate acid chlorides or ethyl chloroformate in mild conditions. The products were characterized by spectroscopy (H-1 NMR, C-13 NMR, IR, and HRMS). Some from the synthesized compounds were screened in vitro and in vivo for antibacterial and antifungal activities against a panel of reference strains of microorganisms. The study revealed that ethyl S-(5-mercapto-1,3,4-thiadiazol-2-y1) carbonothioate seems to he the most active and versatile compound against Gram-positive bacteria, Gram-negative bacteria, and plant pathogenic fungi.
引用
收藏
页码:3241 / 3249
页数:9
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