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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:22

Article

Tamboli, Yasinalli¹  Lazzarato, Loretta¹  Marini, Elisabetta¹  Guglielmo, Stefano¹  Novelli, Michela²  Beffy, Pascale³  Masiello, Pellegrino²  Fruttero, Roberta¹  Gasco, Alberto¹ 

[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;   

DOI  :  10.1016/j.bmcl.2012.03.103

来源: Elsevier

【 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.

【 授权许可】

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