Martin Nathaniel I, Derbyshire Emily R, Marletta Michael A
Department of Chemistry, University of California, Berkeley, CA 94720, USA.
Bioorg Med Chem Lett. 2007 Sep 1;17(17):4938-41. doi: 10.1016/j.bmcl.2007.06.039. Epub 2007 Jun 14.
Soluble guanylate cyclase (sGC) is activated by the known benzylindazole derivative YC-1 [1-benzyl-3-(5'-hydroxymethyl-2'-furyl)-indazole]. YC-1 also acts synergistically with CO, activating sGC to a level comparable to that achieved upon binding of nitric oxide, the endogenous activator of sGC. We here describe the synthesis of a YC-1 phosphonate analogue with improved aqueous solubility as well as its effects on sGC.
可溶性鸟苷酸环化酶(sGC)可被已知的苄基吲唑衍生物YC-1 [1-苄基-3-(5'-羟甲基-2'-呋喃基)-吲唑]激活。YC-1还与一氧化碳协同作用,将sGC激活至与内源性激活剂一氧化氮结合时相当的水平。我们在此描述了一种具有改善的水溶性的YC-1膦酸酯类似物的合成及其对sGC的影响。