An Efficient Synthesis of Novel Bioactive Thiazolyl-Phthalazinediones under Ultrasound Irradiation

Fatma S. Elsharabasy, Sobhi M. Gomha, T. Farghaly, Heba S. A. Elzahabi
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引用次数: 10

Abstract

Novel 2-thiazolylphthalazine derivatives were efficiently synthesized under ultrasound irradiation, resulting in high yields and short reaction times after optimization of the reaction conditions. All prepared compounds were fully characterized using spectroscopic methods. They were screened for their antimicrobial activity against Gram-positive and Gram-negative bacteria as well as for antifungal activity. The antimicrobial activity profile of the tested compounds showed some promising results. The potent activity of compounds 4d, 7b (117% zone inhibition) and 7c (105% zone inhibition) against Salmonella sp., exceeding that of the reference drug Gentamycin is particularly noteworthy. In general, the newly synthesized thiazolylphthalazine derivatives showed higher antimicrobial activity against the tested Gram-negative bacteria than against Gram-positive bacteria and fungi.
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超声辐照下高效合成新型生物活性噻唑基-酞嗪二酮
通过优化反应条件,在超声辐照下高效合成了新型2-噻唑基酞菁衍生物,收率高,反应时间短。所有制备的化合物都用光谱方法进行了表征。筛选了它们对革兰氏阳性菌和革兰氏阴性菌的抗菌活性以及抗真菌活性。所测化合物的抗菌活性谱显示出一些令人鼓舞的结果。特别值得注意的是,化合物4d, 7b(117%区抑制)和7c(105%区抑制)对沙门氏菌的活性超过了参考药物庆大霉素。总的来说,新合成的噻唑基酞嗪衍生物对革兰氏阴性菌的抑菌活性高于对革兰氏阳性菌和真菌的抑菌活性。
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