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

被引:16
作者
Elsharabasy, Fatma S. [1 ,2 ]
Gomha, Sobhi M. [3 ]
Farghaly, Thoraya A. [3 ,4 ]
Elzahabi, Heba S. A. [5 ]
机构
[1] Natl Res Ctr, Dept Chem Nat & Microbial Prod, Dokki 12622, Egypt
[2] Sattam bin Abdul Aziz Univ, Coll Sci & Humanities, Alkharj City 11942, Saudi Arabia
[3] Cairo Univ, Dept Chem, Fac Sci, Giza 12613, Egypt
[4] UmmAl Qura Univ, Fac Sci Appl, Dept Chem, Makkah El Mukarramah 21514, Saudi Arabia
[5] Al Azhar Univ, Fac Pharm Girls, Dept Pharmaceut Chem, Cairo 11754, Egypt
关键词
thiazolylphthalazinediones; hydrazonoyl chlorides; ultrasound irradiation; antimicrobial activity; PHARMACOLOGICAL EVALUATION; BIOLOGICAL-ACTIVITY; DERIVATIVES; THIADIAZOLES; AGENTS; ACID;
D O I
10.3390/molecules22020319
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
引用
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页数:15
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