Antibacterial and antifungal properties of guanylhydrazones

A series of novel guanylhydrazones were designed, synthesized and characterized. All the compounds were screened for their antibacterial and antifungal activity. Compounds 26 and 27 showed excellent antibacterial activities against Staphylococcus aureus ATCC 25923 and Micrococcus luteus ATCC 379 with minimal inhibitory concentrations of 4 ae g mL(-1), and good antifungal activity against Candida parapsilosis ATCC 22019. These results suggested that the selected guanylhydrazones could serve as promising leads for improved antimicrobial development

Synthesis and anti-Candida activity of novel benzothiepino[3,2-c]pyridine derivatives

A novel series of thiepine derivatives were synthesized and evaluated as potential antimicrobials. All the synthesized compounds were evaluated for their antimicrobial activities in vitro against the fungi Candida albicans (ATCC 10231), C.parapsilosis (clinical isolate), Gram-negative bacterium Pseudomonas aeruginosa (ATCC 44752), and Gram-positive bacterium Staphylococcus aureus (ATCC 25923). Synthesized compounds showed higher antifungal activity than antibacterial activity, indicating that they could be used as selective antimicrobials. Selected thiepines efficiently inhibited Candida hyphae formation, a trait necessary for their pathogenicity. Thiepine 8-phenyl[1]benzothiepino[3,2-c]pyridine (16) efficiently killed Candida albicans at 15.6g/mL and showed no embryotoxicity at 75g/mL. Derivative 8-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl][1]benzothiepino[3,2-c]pyridine (23) caused significant hemolysis and in vitro DNA interaction. The position of the phenyl ring was essential for the antifungal activity, while the electronic effects of the substituents did not significantly influence activity. Results obtained from in vivo embryotoxicity on zebrafish (Danio rerio) encourage further structure optimizations

N-Benzyl Derivatives of Long-Chained 4-Amino-7-chloro-quionolines as Inhibitors of Pyocyanin Production in Pseudomonas aeruginosa

Pseudomonas aeruginosa is a leading cause of nosocomial infections that are becoming increasingly difficult to treat due to the occurrence of antibiotic resistant strains. Since P. aeruginosa virulence is controlled through quorum sensing, small molecule treatments inhibiting quorum sensing signaling pathways provide a promising therapeutic option. Consequently, we synthesized a series of N-octaneamino-4-aminoquinoline derivatives to optimize this chemotype's antivirulence activity against P. aeruginosa via inhibition of pyocyanin production. The most potent derivative, which possesses a benzofuran substituent, provided effective inhibition of pyocyanin production (IC50 = 12 mu M), biofilm formation (BFIC50 = 50 mu M), and motility. Experimentally, the compound's activity is achieved through competitive inhibition of PqsR, and structure-activity data were rationalized using molecular docking studies

Using the Behaviour Change Wheel and modified Delphi method to identify behavioural change techniques for improving adherence to smoking cessation medications

Abstract Background Medication adherence is a crucial component of the pharmacological treatment of smoking. Previous interventions targeted to improve adherence to smoking cessation medications (SCMs) were designed using pragmatic approaches. This study aims to develop a comprehensive intervention strategy to improve adherence to SCMs using the Behaviour Change Wheel (BCW) and a modified Delphi method. Methods Recommendations for the design of intervention strategies were based on the BCW guide and six studies conducted by the research team. Factors related to healthcare providers and consumers (person making a quit attempt) that showed associations with adherence were mapped into the Capability, Opportunity, Motivation, Behaviour (COM-B) model, and corresponding intervention functions and policy categories. Interventions were then represented using the Behaviour Change Technique Taxonomy. Finally, a modified Delphi study using 17 experts was conducted to evaluate the nominated strategies using the Acceptability, Practicability, Effectiveness, Affordability, Side-effects, and Equity (APEASE) criteria. Results Following a stepped approach, an adherence support wheel was designed to guide implementation strategies and programmes. Thirteen intervention strategies were selected. The selected interventions include providing detailed instructions on how to use SCMs; establishing realistic expectations from SCMs; and providing training for healthcare providers regarding comprehensive smoking cessation care with specifics on the provision of adherence support. Conclusion The BCW guide and a modified Delphi were applied successfully to design interventions tailored to improve adherence to SCMs. Improving adherence to SCMs requires a comprehensive intervention approach involving various stakeholders. Future research is needed to assess the effectiveness of the nominated intervention strategies