Synthesis of pyochelin–norfloxacin conjugates

Rivault, Freddy; Liébert, Clémence; Burger, Alain; Hoegy, Françoise; Abdallah, Mohamed Abou-Elwafa; Schalk, Isabelle J.; Mislin, Gaëtan L. A.

doi:10.1016/j.bmcl.2006.11.005

Cited by 63 publications

(51 citation statements)

References 23 publications

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“…The use of siderophore-drug conjugates as “Trojan Horse” antibiotics has been reviewed extensively (Miller et al 2009; Miller and Malouin 1993; Miethke and Marahiel 2007; Möllman et al 2009; Roosenberg et al 2000a). This topic has maintained high interest amid current research programs (Braun et al 2008; Miller et al 2009; Möllmann et al 2009; Nolan and Walsh 2008; Rivault et al 2007; Wach et al 2008; Rook 2008). …”

Section: Siderophore-mediated Drug Delivery (“Trojan Horse” Antibiotics)mentioning

confidence: 99%

Is drug release necessary for antimicrobial activity of siderophore-drug conjugates? Syntheses and biological studies of the naturally occurring salmycin “Trojan Horse” antibiotics and synthetic desferridanoxamine-antibiotic conjugates

et al. 2009

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The recent rise in drug resistance found amongst community acquired infections has sparked renewed interest in developing antimicrobial agents that target resistant organisms and limit the natural selection of immune variants. Recent discoveries have shown that iron uptake systems in bacteria and fungi are suitable targets for developing such therapeutic agents. The use of siderophore-drug conjugates as "Trojan Horse" drug delivery agents has attracted particular interest in this area. This review will discuss efforts in our research group to study the salmycin class of "Trojan Horse" antibiotics. Inspired by the natural design of the salmycins, a series of desferridanoxamine-antibiotic conjugates were synthesized and tested in microbial growth inhibition assays. The results of these studies will be related to understanding the role of drug release in siderophore-mediated drug delivery with implications for future siderophore-drug conjugate design.

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Section: Siderophore-mediated Drug Delivery (“Trojan Horse” Antibiotics)mentioning

confidence: 99%

Is drug release necessary for antimicrobial activity of siderophore-drug conjugates? Syntheses and biological studies of the naturally occurring salmycin “Trojan Horse” antibiotics and synthetic desferridanoxamine-antibiotic conjugates

et al. 2009

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“…Recently, different pyochelin-norfloxacin conjugates were tested against P. aeruginosa. Two out of four showed bactericidal activity, those containing a labile spacer, presumably due to better antibiotic dissociation in vivo (Rivault et al, 2007). So far no ornibactin-antibiotic conjugates have been synthesized and tested against Burkholderia cepacia complex.…”

Section: Therapeutic Interventions Focusing On Siderophore-mediated Imentioning

confidence: 98%

Role of siderophores in cystic fibrosis pathogenesis: Foes or friends?

Mossialos

Amoutzias

2009

International Journal of Medical Microbiology

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“…One possibility is to introduce siderophorelike antibiotics, which may be transported by the bacterial cell, which recognizes the antibiotic as its own siderophore (Budzikiewicz 2001;Braun and Braun 2002). Recently, the synthesis of such compounds, namely pyochelin-norfloxacin conjugates was reported (Rivault et al 2007). Further research is needed in order to assess the bactericidal properties on different P. aeruginosa isolates.…”

Section: The Quest For New Targetsmentioning

confidence: 98%

Towards understanding Pseudomonas aeruginosa burn wound infections by profiling gene expression

et al. 2007

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Pseudomonas aeruginosa is a key opportunistic pathogen causing severe acute and chronic nosocomial infections in immunocompromised or catheterized patients. It is prevalent in burn wound infections and it is generally multi-drug resistant. Understanding the genetic programs underlying infection is essential to develop highly needed new strategies for prevention and therapy. This work reviews expression profiling efforts conducted worldwide towards gaining insights into pathogenesis by P. aeruginosa, in particular in burn wounds. Work on various infection models, including the burned mouse model, has identified several direct virulence factors and elucidated their mode of action. In vivo gene expression experiments using In vivo Expression Technology (IVET) ascertained distinct regulatory circuits and traits that have helped explain P. aeruginosa s success as a general pathogen. The sequencing of the whole genome from a number of P. aeruginosa strains and the construction of genome-wide microarrays have paved the road to the several insightful studies on the (interacting) traits underlying infection. A series of in vitro and initial in vivo gene expression studies revealed specific traits pivotal for infection, such as quorum sensing systems, iron acquisition and oxidative stress responses, and toxin production among others. The data sets obtained from global transcriptional profiling provide insights that will be essential for the development of new targets and options for prevention and intervention.

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Synthesis of pyochelin–norfloxacin conjugates

Cited by 63 publications

References 23 publications

Is drug release necessary for antimicrobial activity of siderophore-drug conjugates? Syntheses and biological studies of the naturally occurring salmycin “Trojan Horse” antibiotics and synthetic desferridanoxamine-antibiotic conjugates

Is drug release necessary for antimicrobial activity of siderophore-drug conjugates? Syntheses and biological studies of the naturally occurring salmycin “Trojan Horse” antibiotics and synthetic desferridanoxamine-antibiotic conjugates

Role of siderophores in cystic fibrosis pathogenesis: Foes or friends?

Towards understanding Pseudomonas aeruginosa burn wound infections by profiling gene expression

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