30189-85-6Relevant academic research and scientific papers
Phenothiazinium-fluoroquinolone drug conjugates
Wainwright, Mark,Shah, Ami,Meegan, Katie,Loughran, Ciara,Smith, Andy,Valli, Nasima,Dempster, Nicola
, p. 405 - 409 (2010)
Synthesis and antibacterial screening of a homologous series of 3-dialkylaminophenothiazinium-7-norfloxacin conjugates was carried out alongside a corresponding series of symmetrical methylene blue derivatives. The norfloxacin conjugates maintained typical methylene blue derivative photoproperties, such as long wavelength absorption, but produced no measurable singlet oxygen in the standard assay and provided no significant increase in the magnitude of photoantibacterial action, this being similar to the methylene blue homologues, although both the conjugates and homologues were considerably more active than methylene blue itself both against Staphylococcus aureus and Escherichia coli. DNA binding via intercalation was considerably greater for the series of norfloxacin conjugates than for the methylene blue homologues.
DEVELOPMENTS IN BIOLOGICALLY ACTIVE METHYLENE BLUE DERIVATIVES (2)
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Page/Page column 25-26, (2010/02/12)
A phenothiazinium compound of Formula (I) for use as an antimicrobial agent for the prevention of microbial infections wherein: Rl, R2, R3 and R4 each independently is an optionally substituted linear, branched or cyclic hydrocarbon group;or Rl and R2 or R3 and R4 together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7- membered ring; XP- is a counteranion; and P is 1, 2 or 3. The invention also relates to compositions comprising phenothiazinium. compounds, to selected compounds and their use as medicaments, as PDT agents, as photodiagnostic agents, to a conjugate or composite formed between a phenothiazinium. and a polymer; and to a method for sterilising fluids in which the fluid is passed over the conjugate or composite whilst it is illuminated. The compounds are biologically active photosensitisers which are strongly photocytotoxic and have application in the areas of photodynamic therapy (PDT), as well as for the diagnosis and detection of medical conditions and related uses in photochemical internalisation, in the production of cancer vaccines, in the treatment and prevention of microbial infections and in photodisinfection or photosterilisation.
