721-01-7Relevant academic research and scientific papers
NOVEL DXR INHIBITORS FOR ANTIMICROBIAL THERAPY
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Page/Page column 69; 74-75, (2011/05/05)
The present invention generally concerns particular methods and compositions for antimicrobial therapy. In particuarl embodiments, the compositions target DXR. In specific embodiments, the compositions are electron-deficient heterocyclic rings.
Coordination chemistry based approach to lipophilic inhibitors of 1-deoxy-D-xylulose-5-phosphate reductoisomerase
Deng, Lisheng,Sundriyal, Sandeep,Rubio, Valentina,Shi, Zheng-Zheng,Song, Yongcheng
supporting information; experimental part, p. 6539 - 6542 (2010/04/04)
1-Deoxy-D-xylulose-5-phosphate reductoisomerase (DXR) in the non-mevalonate pathway found in most bacteria is a validated anti-infective drug target. Fosmidomycin, a potent DXR inhibitor, is active against Gram-negative bacteria. A coordination chemistry and structure based approach was used to discover a novel, lipophilic DXR inhibitor with an IC50 of 1.4 μM. It exhibited a broad spectrum of activity against Gram-negative and -positive bacteria with minimal inhibition concentrations of 20-100 μM (or 3.7-19 μg/mL).
Synthesis of N-1-oxypyrimidine 1,3-dioxolane and 1,3-oxathiolane nucleosides
Nguyen-Ba,Lee,Chan,Zacharie
, p. 2311 - 2312 (2007/10/03)
Two series of 1,3-dioxolanes and 1,3-oxathiolane nucleosides containing N-1-oxypyrimidine were synthesized as potential antiviral agents.
Novel Iron Sequestering Agents: Synthesis and Iron-Chelating Properties of Hexadentate Ligands Composed of 1-Hydroxy-2(1H)-pyrimidinone, ω-Amino Carboxylic Acid, and Tris(2-aminoethyl)amine
Ohkanda, Junko,Kamitani, Jun,Tokumitsu, Takeshi,Hida, Yoko,Konakahara, Takeo,Katoh, Akira
, p. 3618 - 3624 (2007/10/03)
Novel heterocyclic hexadentate ligands (3HOPYn: n = 5-7), in which three units of 1-hydroxy-2(1H)-pyrimidinone are linked to tris(2-aminoethyl)amine through an amide bond by an alkyl chain, were synthesized, and their iron-chelating properties were investigated. The stability of their iron complexes (25 to 27 in log K) was significantly larger than that of pyrazinone-containing ligands by virtue of higher pKa values. On kinetic evaluation of iron removal from human transferrin, 3HOPY5 showed remarkable efficiency over five times as much as commercially available desferrioxamine B. The conformational analysis of the corresponding Ga(III) complex of Fe(opy5) by 1H NMR and by MM and MD calculations are also discussed.
