512125

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Pyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious gram-negative infections.

Justin I Montgomery et al.

Journal of medicinal chemistry, 55(4), 1662-1670 (2012-01-20)

The synthesis and biological activity of a new series of LpxC inhibitors represented by pyridone methylsulfone hydroxamate 2a is presented. Members of this series have improved solubility and free fraction when compared to compounds in the previously described biphenyl methylsulfone

Synthesis of new linear poly(phenylpyridyl) chains

Perato, S.; et al.

Tetrahedron, 68, 1910-1917 (2012)

Design and characterization of optimized adenosine A₂A/A₁ receptor antagonists for the treatment of Parkinson's disease.

Brian C Shook et al.

Journal of medicinal chemistry, 55(3), 1402-1417 (2012-01-14)

The design and characterization of two, dual adenosine A(2A)/A(1) receptor antagonists in several animal models of Parkinson's disease is described. Compound 1 was previously reported as a potential treatment for Parkinson's disease. Further characterization of 1 revealed that it was

Regioselective Suzuki coupling on pyridinium N-(3,5-dibromoheteroar-2-yl)aminides

M. Jose R, et al.

Tetrahedron Letters, 47, 36, 6457-6460 (2006)

Cu(acac)2-catalyzed N-arylations of phenylurea with arylboronic acid

Gavade, S.; et al.

Synthetic Communications, 42, 1704-1714 (2012)

A new access to 3-substituted-1(2H)-isoquinolone by tandem palladium-catalyzed intramolecular aminocarbonylation annulation.

Antoine Dieudonné-Vatran et al.

Organic & biomolecular chemistry, 10(13), 2683-2691 (2012-03-01)

An original tribromide derivative based, palladium-catalyzed synthesis of 3-substituted-1(2H)-isoquinolone is described based on a regioselective Suzuki-Miyaura C-C coupling on o-halo-(2,2-dihalovinyl)-benzene followed by a palladium catalyzed amination-carbonylation-cyclization reaction. This sequence efficiently proceeds to build up isoquinolone in fair to good yields

Phosphine-free Suzuki-Miyaura cross-coupling in aqueous media enables access to 2-C-aryl-glycosides.

Isidro Cobo et al.

Organic letters, 14(7), 1728-1731 (2012-03-14)

A general strategy for the synthesis of 2-aryl-glycals and their elaboration to 2-C-aryl-α-glycosides and 1,5-anhydro-2-C-aryl-2-deoxy alditols are described. The use of reliable, efficient phosphine-free Suzuki-Miyaura cross-coupling of 2-iodoglycals in aqueous media as a key step proceeds with complete regioselectivity at

Copper-mediated sequential cyanation of aryl C-B and arene C-H bonds using ammonium iodide and DMF.

Jinho Kim et al.

Journal of the American Chemical Society, 134(5), 2528-2531 (2012-01-28)

The cyanation of aromatic boronic acids, boronate esters, and borate salts was developed under copper-mediated oxidative conditions using ammonium iodide and DMF as the source of nitrogen and carbon atom of the cyano unit, respectively. The procedure was successfully extended

Structural characterizations of oligopyridyl foldamers, α-helix mimetics.

Jana Sopkova-de Oliveira Santos et al.

Journal of chemical information and modeling, 52(2), 429-439 (2011-12-27)

Protein-protein interactions are central to many biological processes, from intracellular communication to cytoskeleton assembly, and therefore represent an important class of targets for new therapeutics. The most common secondary structure in natural proteins is an α-helix. Small molecules seem to

Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors.

Jianwei Yan et al.

Bioorganic & medicinal chemistry letters, 22(5), 1976-1979 (2012-02-07)

A series of P1-substituted biaryl amprenavir derivatives was designed and synthesized. These compounds were evaluated for enzyme inhibition and antiviral activity in vitro. Several compounds showed highly efficient antiviral activity with EC(50) values down to 0.10nM, which are more potent

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