229307-70-4

Upstream product

• 110-87-2 3,4-dihydro-2H-pyran 
• 229307-69-1 4-Benzhydryloxy-7-((2R,3R,4S,5R)-3-hydroxy-5-methoxy-6,6-dimethyl-4-triethylsilanyloxy-tetrahydro-pyran-2-yloxy)-8-methyl-chromen-2-one 
• 107739-83-3 (+)-6-deoxy-5-C,4-O-dimethyl-L-xylo-hexopyranose 
• 229307-68-0 7-[[6-Deoxy-5-C-methyl-4-O-methyl-α-L-lyxo-hexopyranosyl]oxy]-4-(diphenylmethoxy)-8-methyl-2H-1-benzopyran-2-one 
• 229307-67-9 4-(diphenylmethoxy)-7-hydroxy-8-methyl-2H-1-benzopyran-2-one 

Relevant academic research and scientific papers

Ribose-substituted aromatic amides, method for the production and use thereof as medicaments

Compounds of formula (I); wherein R1=alkyl, alkenyl or alkynyl, O-alkyl, O-alkenyl or optionally substituted, optionally interrupted O-alkynyl; R2=hydrogen or halogen; R3=hydrogen, alkyl or halogen; R4=NHR′ or N

Coumarin inhibitors of gyrase B with N-propargyloxy-carbamate as an effective pyrrole bioisostere

The synthesis and biological profile in vitro of a series of coumarin inhibitors of gyrase B bearing a N-propargyloxycarbamate at C-3' of noviose is presented. Replacement of the 5-methylpyrrole-2-carboxylate of coumarin drugs with an N-propargyloxycarbamate bioisostere leads to analogues with improved antibacterial activity. Analysis of crystal structures of coumarin antibiotics with the 24 kDa N-terminal domain of the gyrase B protein provides a rational for the excellent inhibitory potency of C-3' N- alkoxycarbamates.