Discovery of an orally bioavailable alkyl oxadiazole β3 adrenergic receptor agonist

被引：23

作者：

Feng, DQD ^{[1
]}

Biftu, T

Candelore, MR

Cascieri, MA

Colwell, LF

Deng, LP

Feeney, WP

Forrest, MJ

Hom, GJ

MacIntyre, DE

Miller, RR

Stearns, RA

Strader, CD

Tota, L

Wyvratt, MJ

Fisher, MH

Weber, AE

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Physiol & Biochem, Rahway, NJ 07065 USA

[3] Merck Res Labs, Dept Drug Metab, Rahway, NJ 07065 USA

[4] Merck Res Labs, Dept Pharmacol, Rahway, NJ 07065 USA

[5] Merck Res Labs, Dept Comparat Med, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(00)00267-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-n-Pentyl oxadiazole substituted benzenesulfonamide 8 is a potent and selective beta(3) adrenergic receptor agonist (beta(3) EC50 = 23 nM, beta(1) IC50 = 3000 nM, beta(2) IC50 = 3000 nM). The compound has high oral bioavailability in dogs (62%) and rats (36%) and is among the: most orally bioavailable beta(3) adrenergic receptor agonists reported to date. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1427 / 1429

页数：3

共 17 条

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