Anthony, Nahoum G.; Breen, David; Clarke, Joanna; Donoghue, Gavin; Drummond, Allan J.; Ellis, Elizabeth M.; Gemmell, Curtis G.; Helesbeux, Jean-Jacques; Hunter, Iain S.; Khalaf, Abedawn I.; Mackay, Simon P.; Parkinson, John A.; Suckling, Colin J.; Waigh, Roger D. published the artcile< Antimicrobial Lexitropsins Containing Amide, Amidine, and Alkene Linking Groups>, Category: nitriles-buliding-blocks, the main research area is lexitropsin antibiotic antimicrobial antibacterial agent preparation; distamycin analog lexitropsin antimicrobial antibacterial agent preparation; thiazotropsin analog lexitropsin antimicrobial antibacterial agent prepare; fungicide lexitropsin antimicrobial distamycin analog preparation.
The synthesis and properties of 80 short minor groove binders, such as I, related to distamycin and the thiazotropsins were described. The design of the compounds was principally predicated upon increased affinity arising from hydrophobic interactions between minor groove binders and DNA. The introduction of hydrophobic aromatic head groups, including quinolyl and benzoyl derivatives, and of alkenes as linkers led to several strongly active antibacterial compounds with MIC for Staphylococcus aureus, both methicillin-sensitive and -resistant strains, in the range of 0.1-5 μg mL-1, which is comparable to many established antibacterial agents. Antifungal activity was also found in the range of 20-50 μg mL-1 MIC against Aspergillus niger and Candida albicans, again comparable with established antifungal drugs. A quinoline derivative was found to protect mice against S. Aureus infection for a period of up to six days after a single i.p. dose of 40 mg kg-1.
Journal of Medicinal Chemistry published new progress about Antibacterial agents. 6136-93-2 belongs to class nitriles-buliding-blocks, and the molecular formula is C6H11NO2, Category: nitriles-buliding-blocks.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts