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
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
收藏
页码:3810 / 3815
页数:6
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