Novel derivatives of 5-amino-1-cyclopropyl-7-[(3R,5S)3,5-dimethylpiperazine-1-yl]-6,8-difluoro-4-oxo-quinoline-3-carboxylic acid: their synthesis, antimicrobial, antifungal, and urease inhibitory studies
“…Quinolone derivatives are another interesting class of compounds, due to some of their pharmacological properties [116] , [117] , [118] , [119] ; these compounds were synthesized and screened as urease inhibitors. The studies conducted with sparfloxaxin (Series A, Scheme 43 ) [120] and 8-nitroflouroquinolone (Series B, Scheme 43 ) [121] derivatives revealed moderate urease inhibition activities. Scheme 43 Chemical structures of quinolones described as urease inhibitors.…”
Section: Organic Substances As Urease Inhibitorsmentioning
“…Quinolone derivatives are another interesting class of compounds, due to some of their pharmacological properties [116] , [117] , [118] , [119] ; these compounds were synthesized and screened as urease inhibitors. The studies conducted with sparfloxaxin (Series A, Scheme 43 ) [120] and 8-nitroflouroquinolone (Series B, Scheme 43 ) [121] derivatives revealed moderate urease inhibition activities. Scheme 43 Chemical structures of quinolones described as urease inhibitors.…”
Section: Organic Substances As Urease Inhibitorsmentioning
“…Chymotrypsin inhibitory activity was studied at 410nm by adopting Cannel Method using Chymostatin as standard. Calculations were performed on SoftMax Pro software (Molecular Devices) [ 19 , 20 ].…”
“…The SAR revealed that the linker between the fluoroquinolone and nalidixic acid has great influence on the activity, and hybrids 23b,d with 1,2,4‐triazole‐5(4 H )‐thione as linker were inactive against C. albicans and S. cerevisiae . The sparfloxacin derivatives 24a–c not only showed promising antibacterial activity against a range of Gram‐positive and Gram‐negative pathogens which were comparable to the parent sparfloxacin, but also exhibited considerable antifungal against Fusarium solani , Trichophyton rubrum , Aspergillus parasiticus , C. albicans , and A. effuses , suggesting that the sparfloxacin derivatives 24a–c were more potent than the references sparfloxacin, gatifloxacin, and gemifloxacin against most fungi . However, the norfloxacin‐/ciprofloxacin‐benzimidazole hybrids 25 were inactive against A. niger , R. nigricans , and C. albicans at the concentration of 50 μg/ml…”
More than 300 million people suffer from the incidence of life‐threatening invasive fungal infections, resulting in over 1.35 million deaths annually. Currently, the antifungal agents available in clinics are rather limited, and the rapid development of resistance to the existing antifungal drugs has further aggravated mortality. Quinolones possess a broad spectrum of chemotherapeutic properties and demonstrate considerable antifungal activities as well. Various quinolone derivatives have been screened for their antifungal activities, and some of them exhibit excellent potency against both drug‐susceptible and drug‐resistant fungi. This review aims to outline the recent advances in quinolone derivatives as potential antifungal agents and summarize the structure–activity relationship, to provide insights for the rational design of more active candidates.
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