Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor

Autor: Maloney, Patrick R., Khan, Pasha, Hedrick, Michael, Gosalia, Palak, Milewski, Monika, Li, Linda, Roth, Gregory P., Sergienko, Eduard, Suyama, Eigo, Sugarman, Eliot, Nguyen, Kevin, Mehta, Alka, Vasile, Stefan, Su, Ying, Stonich, Derek, Nguyen, Hung, Zeng, Fu-Yue, Novo, Arianna Mangravita, Vicchiarelli, Michael, Diwan, Jena, Chung, Thomas D.Y., Smith, Layton H., Pinkerton, Anthony B.

Publikováno v: In Bioorganic & Medicinal Chemistry Letters 1 November 2012 22(21):6656-6660

Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces parasite growth in vitro.

Autor: Preuss J; Department of Pediatrics, University of California, San Diego, La Jolla, California 92037, United States., Maloney P, Peddibhotla S, Hedrick MP, Hershberger P, Gosalia P, Milewski M, Li YL, Sugarman E, Hood B, Suyama E, Nguyen K, Vasile S, Sergienko E, Mangravita-Novo A, Vicchiarelli M, McAnally D, Smith LH, Roth GP, Diwan J, Chung TD, Jortzik E, Rahlfs S, Becker K, Pinkerton AB, Bode L

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2012 Aug 23; Vol. 55 (16), pp. 7262-72. Date of Electronic Publication: 2012 Aug 06.