Antimicrobial and Antiquorum-Sensing Studies. Part 3: Synthesis and Biological Evaluation of New Series of [1,3,4]Thiadiazoles and Fused [1,3,4]Thiadiazoles

被引:31
作者
El-Gohary, Nadia S. [1 ]
Shaaban, Mona I. [2 ,3 ]
机构
[1] Mansoura Univ, Fac Pharm, Dept Med Chem, Mansoura 35516, Egypt
[2] Mansoura Univ, Fac Pharm, Dept Microbiol, Mansoura 35516, Egypt
[3] Taibah Univ, Coll Pharm, Dept Microbiol, Almadinah Almunawwarah, Saudi Arabia
关键词
1,3,4]Thiadiazoles; Fused [1,3,4]thiadiazoles; Antimicrobial activity; Antiquorum-sensing activity; Cytotoxic activity; In vivo acute toxicity; In silico studies; AERUGINOSA BIOFILM FORMATION; MESOIONIC PURINONE ANALOGS; RAPID COLORIMETRIC ASSAY; ANTIBACTERIAL ACTIVITY; CYTOTOXIC ACTIVITIES; CELL COMMUNICATION; SWARMING MOTILITY; QUORUM; DERIVATIVES; ANTITUMOR;
D O I
10.1002/ardp.201400381
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
New series of [1,3,4]thiadiazoles and fused [1,3,4]thiadiazoles were synthesized. The newly synthesized compounds were screened for their antibacterial activity against Staphylococcus aureus, Bacillus cereus, and Escherichia coli. Compounds 3b and 10a displayed the highest activity against E. coli with MIC value of 78.125g/mL. In addition, compound 10a exhibited the highest activity against B. cereus with MIC value of 156.25g/mL. The antifungal activity of these compounds was also tested against Candida albicans and Aspergillus flavus 3375. Compounds 3b, 5a, 10a, and 12b showed the best activity against A. flavus 3375 with MIC value of 19.531g/mL. The same compounds were examined for their antiquorum-sensing activity against Chromobacterium violaceum ATCC 12472, whereas compounds 3b, 5a, and 12b exhibited moderate activity. In vitro cytotoxicity testing of compounds 3b,c, 5a, 6a, 10a, and 12a,b against human normal lung fibroblast (W138) cell line was performed. The in vivo acute toxicity of the same compounds was also tested and the obtained results indicated that compound 10a is the least toxic analog. The same compounds were studied for their DNA-binding affinity and the obtained results showed that compounds 3b, 10a, and 12a,b have moderate DNA-binding affinity.
引用
收藏
页码:283 / 297
页数:15
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