Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 5-Chloropicolinaldehyde, is researched, Molecular C6H4ClNO, CAS is 31181-89-2, about Discovery of thiosemicarbazone derivatives as effective New Delhi metallo-β-lactamase-1 (NDM-1) inhibitors against NDM-1 producing clinical isolates.Recommanded Product: 5-Chloropicolinaldehyde.
In this study, structure-activity relationship based on thiosemicarbazone derivatives (E)-R1C(S)NHN=C(R2)(R3) (I) (R1 = phenylamino, Ph, cyclohexylamino, morpholin-4-yl, etc.; R2 = H, Me; R3 = Ph, pyridin-2-yl, 3,4,5-trimethoxyphenyl, etc.) was systematically characterized and their potential activities combined with meropenem (MEM) were evaluated. Compounds (I).HCl [R1 = piperazin-1-yl, R2 = H, R3 = 2-hydroxyphenyl (II); R1 = 4-methylpiperazin-1-yl, R2 = H, R3 = 2-hydroxyphenyl (III)] exhibited excellent activity against 10 NDM-pos. isolate clin. isolates in reversing MEM resistance. Further studies demonstrated that compounds II and III were uncompetitive NDM-1 inhibitors with Ki = 0.63 and 0.44μmol/L, resp. Mol. docking speculated that compounds II and III were most likely to bind in the allosteric pocket which would affect the catalytic effect of NDM-1 on the substrate meropenem. Toxicity evaluation experiment showed that no hemolysis activities were found even at concentrations of 1000 mg/mL against red blood cells. In vivo exptl. results showed that a combination of MEM and compound III was markedly effective in treating infections caused by NDM-1 pos. strain and prolonging the survival time of sepsis mice. The finding showed that compound III might be a promising lead in developing new inhibitor to treat NDM-1 producing superbug.
In some applications, this compound(31181-89-2)Recommanded Product: 5-Chloropicolinaldehyde is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.
Reference:
Phosphine ligand,
Chiral phosphine ligands in asymmetric synthesis. Molecular structure and absolute configuration of (1,5-cyclooctadiene)-(2S,3S)-2,3-bis(diphenylphosphino)butanerhodium(I) perchlorate tetrahydrofuran solvate