5 research outputs found
Synthesis and antimicrobial evaluation of new nitric oxideâdonating fluoroquinolone/oxime hybrids
No full textA new series of nitric oxideâdonating fluoroquinolone/oximes was prepared in this study. The nitric oxide release from the prepared compounds was measured using a modified Griess colorimetric method. The antitubercular evaluation of the synthesized compounds indicated that ketone derivatives 2b and 2e and oximes 3b and 3d exhibited somewhat higher activity than their respective parent fluoroquinolones. Mycobacterial DNA cleavage studies and molecular modeling of Mycobacterium tuberculosis DNA gyrase were pursued to explain the observed bioactivity. More important, antibacterial evaluation showed that oximes 3câe are highly potent against Klebsiella pneumoniae, with minimum inhibitory concentration (MIC) values of 0.06, 0.08, and 0.034â”M, respectively, whereas ketone 2c and oxime 4c are more active against Staphylococcus aureus than ciprofloxacin (MIC values: 0.7, 0.38, and 1.6â”M, respectively). Notably, the antipseudomonal activities of compounds 2a and 4c were much higher than those of their respective parent fluoroquinolones
New fluoroquinolones/nitric oxide donor hybrids: design, synthesis and antitubercular activity
No full textNew nitric oxide (NO) donating fluoroquinolones/nitrate ester hybrids were prepared and their structures were characterizedby various spectroscopic and analytical tools. The release of NO from the prepared nitrate esters was measured using the modified Griess colorimetric method. Evaluation of antitubercular activity showed that most of tested compounds exhibited comparable or higher activity than the parent fluoroquinolones. Compounds 2b, 3a, 4a, 5a, and 2d showed better activity than ciprofloxacin. Nevertheless, none of the new compounds were superior to the parent fluoroquinolones in terms of DNA cleavage stimulation in mycobacteria. The additional growth inhibition effect that is distinct from gyrase poisoning may be due to release of NO or enhancement of lipophilicity. These data are augmented by docking results where the docked compounds did not exert additional significant bindings over the parent fluoroquinolones
Experiences and unmet needs among caregivers of children living with autism spectrum disorder in Nigeria: a qualitative study using the socio-ecological model
Get PDFAbstract Introduction This study examines the experiences and unmet needs of caregivers of children with autism spectrum disorder in Nigeria. With a high prevalence in Nigeria, autism spectrum disorder poses a heavy economic burden on society and the patientsâ families, with limited social interactions and stigma. Despite this, the unmet needs and psychosocial burdens of autism spectrum disorder on caregivers have been understudied in Nigeria. The study contributes evidence and raises interest in this area of research. Methods This qualitative study was conducted among twenty-three purposively selected caregivers. Questions from the PREPARE and Zarit Burden Interview tools were adapted for the interview and discussion guides. Data were collected among caregivers of pupils in selected special needs schools in Cross River State, Nigeria. Inductive and deductive approaches were used for the analysis using NVivo 20 pro. The socio-ecological model was used to generate the themes and quotes. Results The study generated four themes and eleven sub-themes across four levels of the socio-ecological model. Findings from our study showed that caregivers of children undergo significant emotional distress, disbelief, and fear at the early stage of diagnosis. Furthermore, families and friends had difficulty comprehending or accepting their childrenâs diagnosis, which further created tension and misunderstanding. Socio-cultural contexts such as stigma and isolation were not uncommon in the society. Conclusion Given the burden of the psychological demand and stigma attached to caregivers and children with autism, there is an urgent need for a tailor-made intervention with the key interplay of individual, interpersonal, societal/institutional, and policy in Nigeria. Advocacy efforts and awareness chaired by caregivers should be strengthened across all levels of the society in Nigeria
Voices from 'Ground Zero':Interrogating History, Culture and Identity in the Resolution of Cameroon's Anglophone Conflict
Get PDFDesign, synthesis and molecular docking of new N-4-piperazinyl ciprofloxacin-triazole hybrids with potential antimicrobial activity
No full textNew N-4-piperazinyl ciprofloxacin-triazole hybrids 6a-o were prepared and characterized. The in vitro antimycobacterial activity revealed that compound 6a experienced promising antimycobacterial activity against Mycobactrium smegmatis compared with the reference isoniazide (INH). Additionally, compound 6a exhibited broad spectrum antibacterial activity against all the tested strains either Gram-positive or Gram-negative bacteria compared with the reference ciprofloxacin. Also, compounds 6g and 6i displayed considerable antifungal activity compared with the reference ketoconazole. DNA cleavage assay of the highly active compounds 6c and 6h showed a good correlation between the Mycobactrium cleaved DNA gyrase assay and their in vitro antimycobactrial activity. Moreover, molecular modeling studies were done for the designed ciprofloxacin derivatives to predict their binding modes towards Topoisomerase II enzyme (PDB: 5bs8)
