Metabolites of orally active NO-independent pyrazolopyridine stimulators of soluble guanylate cyclase

被引：64

作者：

Straub, A

Benet-Buckholz, J

Fröde, R

Kern, A

Kohlsdorfer, C

Schmitt, P

Schwarz, T

Siefert, HM

Stasch, JP

机构：

[1] Bayer AG, Pharma Res Ctr, Inst Med Chem, D-42096 Wuppertal, Germany

[2] Bayer AG, Cent Res, Div Struct Res, D-51368 Leverkusen, Germany

[3] Bayer AG, Pharma Res Ctr, Dept Drug Metab & Isotope Chem, D-42096 Wuppertal, Germany

[4] Bayer AG, Pharma Res Ctr, Dept Preclin Pharmacokinet, D-42096 Wuppertal, Germany

[5] Bayer AG, Pharma Res Ctr, Inst Cardiovasc Res, D-42096 Wuppertal, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 06期

关键词：

D O I：

10.1016/S0968-0896(02)00034-2

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The pyrazolopyridine stimulators of soluble guanylate cyclase BAY 41-2272 and 41-8543 were oxidised in rats and dogs at their 5-pyrimidinyl-cyclopropyl and -morpholino residue. These metabolites activate the soluble guanylate cyclase, induce vaso-elaxation and thereby may contribute to the in vivo activity of BAY 41-2272 and BAY 41-8543. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1711 / 1717

页数：7

共 41 条

[1] DIRECT DERIVATIZATION OF GLYOXAL INTO CHIRAL TEMPLATES PROVIDING COMPLETE DISCRIMINATION BETWEEN THE ALDEHYDE GROUPS [J].