Synthesis and preliminary biological profile of new NO-donor tolbutamide analogues

被引：24

作者：

Tamboli, Yasinalli ^{[1
]}

Lazzarato, Loretta ^{[1
]}

Marini, Elisabetta ^{[1
]}

Guglielmo, Stefano ^{[1
]}

Novelli, Michela ^{[2
]}

Beffy, Pascale ^{[3
]}

Masiello, Pellegrino ^{[2
]}

Fruttero, Roberta ^{[1
]}

Gasco, Alberto ^{[1
]}

机构：

[1] Univ Turin, Dipartimento Sci & Tecnol Farmaco, I-10125 Turin, Italy

[2] Univ Pisa, Scuola Med, Dipartimento Patol Sperimentale Biotecnol Med Inf, I-56126 Pisa, Italy

[3] CNR, Ist Fisiol Clin, Area Ric, I-56127 Pisa, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 11期

关键词：

Diabetes mellitus; NO-donor; Multitarget drugs; Anti-aggregatory activity; Insulin release; NITRIC-OXIDE; DERIVATIVES; RESISTANCE; SECRETION; MORTALITY;

D O I：

10.1016/j.bmcl.2012.03.103

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We describe a new class of NO-donor hypoglycemic products obtained by joining tolbutamide, a typical hypoglycemic sulfonylurea, with a NO-donor moiety through a hard link. As NO-donors we chose either furoxan (1,2,5-oxadiazole 2-oxide) derivatives or the classical nitrooxy function. A preliminary biological characterization of these compounds, including stimulation of insulin release from cultured rat pancreatic beta-cells and in vitro vasodilator and anti-aggregatory activities, is reported. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：3810 / 3815

页数：6

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