Synthesis and Antimicrobial Evaluation of Some New 1,2-Bis-(2-(<i>N</i>-arylimino)-1,3-thiazolidin-3-yl)ethane Derivatives
作者:Kamal Mohamed Dawood、Hussein Khalaf-Allah Abu-Deif
DOI:10.1248/cpb.c14-00031
日期:——
antimicrobial activity against four fungi, two Gram-positive and two Gram-negative bacteria and showed high antibacterial and antifungal activities against all the test microorganisms except Pseudomonas aeruginosa and Candida albicans. Compounds 5b, 15b and 19a exhibited the highest activities against the test microorganisms. The MIC evaluation showed that compound 15b has higher activity than Amphotericin
合成了N,N′-二芳基乙烯-双硫脲衍生物1和8,它们与with酰氯的反应产生了相应的双-(2-(N-芳基氨基)-1,3-噻唑烷衍生物5a-d和11a-c。化合物1与几种α-卤代酮的反应得到双-(5-甲基-2-(N-苯基亚氨基)-1,3-噻唑烷衍生物15a-c和19a,b。测试了新合成的化合物的抗菌性对四种真菌,两种革兰氏阳性细菌和两种革兰氏阴性细菌具有较高的活性,对除铜绿假单胞菌和白色念珠菌以外的所有测试微生物均显示出较高的抗菌和抗真菌活性,化合物5b,15b和19a的活性最高。MIC评价显示,化合物15b对所有测试的真菌和革兰氏阳性细菌(葡萄球菌肺炎)具有比两性霉素B和氨苄青霉素更高的活性,并且显示出与氨苄西林类似的对革兰氏阴性细菌(大肠杆菌)的活性。