Design and synthesis of novel bis-oximinoalkanoic acids as potent PPARα agonists

被引：6
|
作者：
Pingali, Harikishore [1 ,2 ]
Jain, Mukul [1 ]
Shah, Shailesh [2 ]
Zaware, Pandurang [1 ]
Makadia, Pankaj [1 ]
Pola, Suresh [1 ]
Thube, Baban [1 ]
Patel, Darshit [1 ]
Patil, Pravin [1 ]
Priyadarshini, Priyanka [1 ]
Suthar, Dinesh [1 ]
Shah, Maanan [1 ]
Giri, Suresh [1 ]
Patel, Pankaj [1 ]
机构：
[1] Zydus Res Ctr, Ahmadabad 382210, Gujarat, India
[2] Maharaja Sayajirao Univ Baroda, Fac Sci, Dept Chem, Vadodara 390002, Gujarat, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 03期
关键词：
Type; 2; diabetes; PPAR alpha agonist; Oximinoalkanoic acids; PPAR alpha/gamma dual agonist; ACTIVATED-RECEPTOR-ALPHA; HYPOLIPIDEMIC AGENTS; INSULIN SENSITIVITY; GAMMA; DERIVATIVES; DISCOVERY; (PPAR)-ALPHA; METABOLISM; MODULATION; GLUCOSE;
D O I：
10.1016/j.bmcl.2009.12.022
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Bis-oximinoalkanoic acid derivatives were designed and synthesized to aid in the characterization of selective PPAR alpha agonists by replacing the oxazole ring with flexible oximino group in the lipophilic tail part of a previously reported compound 3. Selected compounds 9d and 9m showed excellent potency and high selectivity towards PPAR alpha in vitro. These compounds found effective in reducing serum triglycerides (TG) in vivo. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1156 / 1161
页数：6
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