Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues
作者
ROSEN MARK D; VENKATESAN HARIHARAN; PELTIER HILLARY M; BEMBENEK SCOTT D; KANELAKIS KIMON C; ZHAO LUCY X; LEONARD BARRY E; HOCUTT FRANCES M; WU XIAODONG; PALOMINO HEATHER L; BRONDSTETTER THERESA I; HAUGH PETER V; CAGNON LAURENCE; YAN WEN; LIOTTA LISA A; YOUNG ANDREW; MIRZADEGAN TARA; SHANKLEY NIGEL P; BARRETT TERRANCE D; RABINOWITZ MICHAEL H
[摘要]：HIF prolyl 4-hydroxylases (PHD) are a family of enzymes that mediate key physiological responses to hypoxia by modulating the levels of hypoxia inducible factor 1-alpha (HIF1 alpha). Certain benzimidazole-2-pyrazole carboxylates were discovered to be PHD2 inhibitors using ligand- and structure-based methods and found to be potent, orally efficacious stimulators of erythropoietin secretion in vivo.
