Search results for "Tetronic acid"

showing 2 items of 2 documents

Synthesis, biological evaluation, and molecular docking studies of aldotetronic acid-based LpxC inhibitors

2022

: In order to develop novel inhibitors of the bacterial deacetylase LpxC bearing a substituent to target the UDP binding site of the enzyme, a series of aldotetronic acid-based hydroxamic acids was accessed in chiral pool syntheses starting from 4,6-O-benzylidene-d-glucose and l-arabinitol. The synthesized hydroxamic acids were tested for LpxC inhibitory activity in vitro, revealing benzyl ether 17a ((2S,3S)-4-(benzyloxy)-N,3-dihydroxy-2-[(4-{[4-(morpholinomethyl)phenyl]ethynyl}benzyl)oxy]butanamide) as the most potent LpxC inhibitor. This compound was additionally tested for antibacterial activity against a panel of clinically relevant Gram-negative bacteria, bacterial uptake, and suscepti…

AntibioticsBacterial uptakeLpxC inhibitorsOrganic ChemistryDrug DiscoveryAldotetronic acid derivativesMolecular-docking studiesLasBMolecular BiologyBiochemistrySettore CHIM/08 - Chimica Farmaceutica
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(2S,3′S,3a'R,5′R,7a'R)-5′-[(E)-5-(Furan-3-yl)-2-methylpent-1-en-1-yl]-3-hydroxy-3′,4,7′-trimethyl-1′,2′,3′,3a',5′,7a'-hexahydro-5H-spiro[furan-2,4′-i…

2020

The title compound, ircinianin, C25H32O4, belongs to the sesterterpene tetronic acid compound family and was isolated from the marine sponge Ircinia wistarii. These chemical scaffolds are pharmacologically relevant, since they represent a new class of glycine receptor modulators. The furan ring makes a dihedral angle of 35.14 (12)° to the 4-hydroxy-3-methylfuran-2(5H)-one ring. The crystal packing is characterized by intermolecular O—H...O hydrogen bonds, which generate [010] chains.

Natural productbiology010405 organic chemistryStereochemistryHydrogen bondCrystal structureDihedral angle010402 general chemistryRing (chemistry)biology.organism_classification01 natural sciences0104 chemical scienceschemistry.chemical_compoundchemistryFuranIrciniaTetronic acidIUCrData
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