Synthesis and antihyperglycemic activity profiles of novel thiazolidinedione derivatives

被引：52
作者：
Bhat, BA
Ponnala, S
Sahu, DP [1 ]
Tiwari, P
Tripathi, BK
Srivastava, AK
机构：
[1] Cent Drug Res Inst, Div Med & Proc Chem, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, Div Biochem, Lucknow 226001, Uttar Pradesh, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2004年 / 12卷 / 22期
关键词：
antihyperglycemic activity; thiazolidinedione; diabetes; SLM; PPAR gamma;
D O I：
10.1016/j.bmc.2004.08.031
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A number of thiazolidine-2,4-diones derivatives having carboxylic ester appendage at N-3 were synthesized and their antihyperglycemic activity was evaluated. Many of these derivatives as well as their corresponding carboxylic acid showed significant improvement on post-prandial hyperglycemia in normal rats, in contrast to their poor agonist activity at PPARgamma. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5857 / 5864
页数：8
相关论文
共 16 条
[1]   Drug therapy - Metformin [J].
Bailey, CJ ;
Turner, RC .
NEW ENGLAND JOURNAL OF MEDICINE, 1996, 334 (09) :574-579
[2]   Synthesis and aldose reductase inhibitory activity of 5-arylidene-2,4-thiazolidinediones [J].
Bruno, G ;
Costantino, L ;
Curinga, C ;
Maccari, R ;
Monforte, F ;
Nicolò, F ;
Ottanà, R ;
Vigorita, MG .
BIOORGANIC & MEDICINAL CHEMISTRY, 2002, 10 (04) :1077-1084
[3]   [[OMEGA-(HETEROCYCLYLAMINO)ALKOXY]BENZYL]-2,4-THIAZOLIDINEDIONES AS POTENT ANTIHYPERGLYCEMIC AGENTS [J].
CANTELLO, BCC ;
CAWTHORNE, MA ;
COTTAM, GP ;
DUFF, PT ;
HAIGH, D ;
KINDLEY, RM ;
LISTER, CA ;
SMITH, SA ;
THURLBY, PL .
JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (23) :3977-3985
[4]  
Castaner J., 1987, DRUGS FUTURE, V12, P336
[5]   A new thiazolidinedione, NC-2100, which is a weak PPAR-γ activator, exhibits potent antidiabetic effects and induces uncoupling protein 1 in white adipose tissue of KKAy obese mice [J].
Fukui, Y ;
Masui, S ;
Osada, S ;
Umesono, K ;
Motojima, K .
DIABETES, 2000, 49 (05) :759-767
[6]  
Ginsberg H, 1999, J CARDIOVASC RISK, V6, P337
[7]   SULFONYLUREAS IN NIDDM [J].
GROOP, LC .
DIABETES CARE, 1992, 15 (06) :737-754
[8]   Diabetes and cardiovascular disease - A statement for healthcare professionals from the American Heart Association [J].
Grundy, SM ;
Benjamin, IJ ;
Burke, GL ;
Chait, A ;
Eckel, RH ;
Howard, BV ;
Mitch, W ;
Smith, SC ;
Sowers, JR .
CIRCULATION, 1999, 100 (10) :1134-1146
[9]  
King H, 1998, DIABETES CARE, V21, pB9
[10]   Novel euglycemic and hypolipidemic agents. 4. Pyridyl- and quinolinyl-containing thiazolidinediones [J].
Lohray, BB ;
Bhushan, V ;
Reddy, AS ;
Rao, PB ;
Reddy, NJ ;
Harikishore, P ;
Haritha, N ;
Vikramadityan, RK ;
Chakrabarti, R ;
Rajagopalan, R ;
Katneni, K .
JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (14) :2569-2581
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