title: Novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs as antibacterial agents: a structural activity relationship.
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.
authors: Al-Azhr University, Faculty of Science, Department of Botany and Microbiology, Cairo, Egypt.
authors: Warda A
authors: WA
authors: Hussin
authors: Mohamed A
authors: MA
authors: Ismail
authors: Wael M
authors: WM
authors: El-Sayed
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001372:Aza Compounds / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D004352:Drug Resistance, Microbial; D004357:Drug Synergism; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D013752:Tetracycline / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D001372:Aza Compounds; D013752:Tetracycline
keywords: fractional inhibitory concentration; post-antibiotic effect; resistant variants; synergic interaction
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