Alkene synthesis by isomerization - Organic chemistry
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Low-Molecular-Weight Heparin versus a Coumarin for …
10.1021/ja0749993 - American Chemical Society
As rodents have developed resistance to existing rodenticides, there is a continuous need to develop new and potentially more toxic rodenticides. There are currently three active ingredients belonging to the coumarin rodenticide family registered for use in Florida: brodifacoum, bromadiolone, and warfarin. Brodifacoum was first registered in 1979. It is registered for controlling rats and mice in and around structures, households, industrial sites, and transportation vehicles including trucks, ships, and airplanes. Brodifacoum products are available to the general public and applications may be made as often as necessary. Its mechanism of action is an anticoagulant, and it is absorbed through the gut, inhibiting vitamin K-dependent steps in the synthesis of multiple clotting factors.
General & Introductory Chemistry
Antimicrobial peptides (AMPs) arecurrently being investigatedas potential sources of novel therapeutics against an increasing numberof microorganisms resistant to conventional antibiotics. The conjugationof an AMP to other bioactive compounds is an interesting approachfor the development of new derivatives with increased antimicrobialefficiency and broader spectra of action. In this work, the synthesisof a new peptide–coumarin conjugate via copper(I)-catalyzedazide–alkyne cycloaddition is described. The conjugate wasassayed for in vitro cytotoxicity and displayed antifungalactivity against Cryptococcus gattii and Cryptococcus neoformans. Additionally, the conjugate exhibitedincreased antifungal efficacy when compared with the individual peptide,coumarin, or triazole moieties. Treatment of C. gattii with the peptide–coumarin conjugate enhancedthe production of reactive oxygen species, suggesting that the oxidativeburst plays an important role in the mechanism of action of the conjugate.