1281884-94-3Relevant academic research and scientific papers
Synthesis and antibacterial activity of catecholate-ciprofloxacin conjugates
Fardeau, Sylvain,Dassonville-Klimpt, Alexandra,Audic, Nicolas,Sasaki, Andre,Pillon, Marine,Baudrin, Emmanuel,Mullie, Catherine,Sonnet, Pascal
, p. 4049 - 4060 (2014)
The development of an efficient route to obtain artificial siderophore-antibiotic conjugates active against Gram-negative bacteria is crucial. Herein, a practical access to triscatecholate enterobactin analogues linked to the ciprofloxacin along with their antibacterial evaluation are described. Two series of conjugates were obtained with and without a piperazine linker which is known to improve the pharmacokinetics profile of a drug. A monocatecholate-ciprofloxacin conjugate was also synthesized and evaluated. The antibacterial activities against Pseudomonas aeruginosa for some conjugates are related to the iron concentration in the culture medium and seem to depend on the bacterial iron uptake systems.
Synthesis and Antimicrobial Properties of a Ciprofloxacin and PAMAM-dendrimer Conjugate
Christensen, J?rn Bolstad,Counil, Claire,Ficker, Mario,Frederiksen, Rikki Franklin,Leisner, J?rgen J.,Svenningsen, S?ren Wedel
, (2020)
Infections caused by bacteria resistant to antibiotics are an increasing problem. Multivalent antibiotics could be a solution. In the present study, a covalent conjugate between Ciprofloxacin and a G0-PAMAM dendrimer has been synthesized and tested against clinically relevant Gram-positive and Gram-negative bacteria. The conjugate has antimicrobial activity and there is a positive dendritic effect compared to Ciprofloxacin itself.
Optimizing solubility and permeability of a biopharmaceutics classification system (BCS) class 4 antibiotic drug using lipophilic fragments disturbing the crystal lattice
Tehler, Ulrika,Fagerberg, Jonas H.,Svensson, Richard,Larhed, Mats,Artursson, Per,Bergstr?m, Christel A. S.
, p. 2690 - 2694 (2013/05/21)
Esterification was used to simultaneously increase solubility and permeability of ciprofloxacin, a biopharmaceutics classification system (BCS) class 4 drug (low solubility/low permeability) with solid-state limited solubility. Molecular flexibility was i
