Title |
Novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs as antibacterial agents: a structural activity relationship
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Published in |
Drug Design, Development and Therapy, March 2013
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DOI | 10.2147/dddt.s42073 |
Pubmed ID | |
Authors |
Warda A Hussin, Mohamed A Ismail, Wael M El-Sayed |
Abstract |
Antibiotic resistance is a major health problem; therefore, new antibacterial agents will need to be continuously developed. A series of novel bichalcophenes has been tested and found to have antimicrobial activity against selected bacteria. Due to the promising antimicrobial effects of these 4-substituted phenyl bichalcophene derivatives, the study reported here was launched to examine the interaction between novel bichalcophenes and tetracycline. The minimum inhibitory concentration values for all bichalcophenes were between 8 and 64 μM. Many of the bichalcophenes had synergistic activity that increased the inhibitory effect of tetracycline against bacterial growth, as indicated by the fractional inhibitory concentration index. The post-antibiotic effects of the novel bichalcophenes were determined. Many bichalcophenes were able to elongate the period required for bacteria to recover and grow after a brief exposure to tetracycline. Escherichia coli did not develop resistance to many bichalcophenes over a period of 7 days. A structural activity relationship could be characterized, as monocationic derivatives were more active than the corresponding mononitriles. The presence of a pyridyl group and/or furan ring reduced the activity, while the presence of a phenyl or thiophene ring enhanced the antibacterial activity. Our results suggest that bichalcophenes could be useful to elevate the shelf life of many antibiotics. |
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Geographical breakdown
Country | Count | As % |
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Unknown | 16 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
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Student > Bachelor | 2 | 13% |
Student > Ph. D. Student | 2 | 13% |
Student > Master | 2 | 13% |
Professor | 1 | 6% |
Other | 1 | 6% |
Other | 2 | 13% |
Unknown | 6 | 38% |
Readers by discipline | Count | As % |
---|---|---|
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Chemistry | 2 | 13% |
Biochemistry, Genetics and Molecular Biology | 1 | 6% |
Computer Science | 1 | 6% |
Other | 1 | 6% |
Unknown | 4 | 25% |