The purpose of the study is to assess the effect of a novel quorum sensing inhibitor (QSI), coded as 'yd 47', against otitis media and biofilm formation on Cochlear implants (CIs). Small pieces cut from cochlear implant were implanted under the skin in the retroauricular area on both sides of four guinea pigs. The implant pieces in the study and control sides were implanted in Streptococcus pneumoniae strain solution and saline, respectively. The right and left middle ears were also instilled with a solution containing pneumococci and saline, respectively. The animals were only given an intraperitoneal 'yd 47' twice daily for three months to be assessed later with electron microscopy. Clinical examination with palpation, inspection and otoscopy did not reveal any sign of implant infection or otitis media. In the study and control implant materials, soft tissues around the implant and tympanic membranes, there was no biofilm formation by pneumococci. Contamination by various cells and some rod-shaped bacteria (not diplococcic) were seen in some of the materials. In conclusion, the novel QSI seems promising in the prevention of otitis media and biofilm formation on CIs by pneumococci.
In this study for developing potent analgesic and anti-inflammatory compounds, we synthesized 6-acyl-2-benzoxazolinone and 6-acyl-2-benzothiazolinone derivatives with acetic acid and propanoic acid side chain, and performed preliminary screening of their in vivo analgesic and anti-inflammatory activities at a single dose of 100 mg/kg inmice by a p-benzoquinone-induced writhing test and a Carrageenaninduced hind paw edema model, respectively. We also determined their gastric ulceration effects in the tested animals. Propanoic acid derivatives were generally found to have higher analgesic and anti-inflammatory activities, and among them, 3-(6-benzoyl-2-benzothiazolinon-3-yl)propanoic acid (Compound 4 a) exhibited the highest analgesic and anti-inflammatory activity. However, all compounds showed lower anti-inflammatory effects than we observed for indomethacin at 10 mg/kg dose. Consequently, 6-acyl-2-benzoxazolinone/2-benzothiazolinones having propanoic acid side chain might lead to further studies for developing better candidates with potent analgesic and anti-inflammatory effects while acetic acid derivatives do not exhibit comparable satisfactory features.
It is known that some addition products of beta-nitrostyrenes exhibit potent antimicrobial activity. In order to investigate the effects of structural modifications on the biological properties, some new Michael type addition products of beta-ethyl-beta-nitrostyrenes were synthesized. In this study, eight new 1-[(2-aminophenyl)thio]-1-phenyl-2-nitrobutane (2) derivatives were synthesized by addition of 2-aminothiophenol to the double bond of beta-ethyl-beta-nitrostyrenes (1). The chemical structures were proved by IR and 1H-NMR data and by elemental analysis. Antimicrobial activities of the synthesized compound were investigated against Escherichia coil, Pseudomonas aeruginosa, Proteus mirabilis, Enterococcus faecalis, Bacillus subtilis, Staphylococcus aureus, Candida albicans by the microdilution method. In addition, the newly synthesized compounds were studied for antiviral activities. All of them were found to be almost 100 fold more active than the standard compound aciclovir (CAS 59277-89-3).
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