Synthesis and antihyperglycemic evaluation of new 2,4-thiazolidinediones having biodynamic aryl sulfonylurea moieties

被引：25
作者：
Jawale, Dhanaji V. [1 ]
Pratap, Umesh R. [1 ]
Rahuja, Neha [2 ]
Srivastava, Arvind K. [2 ]
Mane, Ramrao A. [1 ]
机构：
[1] Dr Babasaheb Ambedkar Marathwada Univ, Dept Chem, Aurangabad 431004, Maharashtra, India
[2] Cent Drug Res Inst, Div Biochem, Lucknow 226001, Uttar Pradesh, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 01期
关键词：
2,4-Thiazolidinedione; Sulfonylurea; Antihyperglycemic activity; Curtius rearrangement; Diabetes mellitus; HYPOGLYCEMIC AGENTS; LIPID-METABOLISM; PPAR-GAMMA; FATTY RATS; THIAZOLIDINEDIONE; GLIBENCLAMIDE; CIGLITAZONE; METFORMIN; ANALOGS; LIGAND;
D O I：
10.1016/j.bmcl.2011.10.110
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
New 2,4-thiazolidinediones with aryl sulfonylurea moieties 8a-h have been synthesized by condensing various substituted sulfonamides and 5-(isocyanatomethyl) thiazolidino-2,4-dione 6. The isocyanomethyl thiazolidinedione was obtained by using the Curtius rearrangement, starting from known 2,4-dioxo-5-thiazolidineacetic acid 4. The newly synthesized compounds 8a-h have been evaluated for the antihyperglycemic activity in normal rats model and among these compounds 8b, 8c, 8e and 8f showed significant antihyperglycemic activity in sucrose loaded rat model. (C) 2011 Elsevier Ltd. All rights reserved.
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收藏
页码：436 / 439
页数：4
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