Reduction of insulin resistance in obese and/or diabetic animals by 5-[4-(1-methylcyclohexylmethoxy)benzyl]-thiazolidine-2,4-dione (ADD-3878, U-63,287, ciglitazone), a new antidiabetic agent

Fujita, Toshio; Sugiyama, Yukiteru; Taketomi, Shigehisa; Sohda, Takashi; Kawamatsu, Yutaka; Iwatsuka, H.; Suzuoki, Z.

doi:10.2337/diabetes.32.9.804

Cited by 123 publications

(62 citation statements)

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“…Ciglitazone (3[-4-(1-methylcyclohexylmethoxy)benzyl]-thiazolidine-2,4-dione) was one of the first thiazolidinediones developed (Fujita et al, 1983); clinical development was discontinued in the late 1980s. Subsequently, troglitazone, pioglitazone, and rosiglitazone were introduced for clinical use.…”

Section: Discussionmentioning

confidence: 99%

Effect of thiazolidinediones on bile acid transport in rat liver

Snow

Moseley

2007

Life Sciences

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Section: Discussionmentioning

confidence: 99%

Effect of thiazolidinediones on bile acid transport in rat liver

Snow

Moseley

2007

Life Sciences

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“…Nichtinsulinotrope und insulinotrope Antidiabetika. Ciglitazons, einem Vorläufer der heutigen Glitazone, beschrieben, die mit einer gleichzeitigen Reduktion der Insulinspiegel einherging [26,27].…”

Section: B) Thiazolidindione (Glitazone)unclassified

Kardiovaskul�re Effekte oraler Antidiabetika

Herrmann

Erbel

Janßen

et al. 2004

Herz

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In the recent years there has been increasing interest in the effects of oral hypoglycemic drugs on the cardiovascular system. This has arisen because of recognitions that thiazolidine-diones, peroxisome proliferators-activated receptor gamma (PPAR-gamma), may have antiatherogenic actions and that sulphonylureas are capable of closing the ATP-dependent potassium channel. PPAR-gamma agonists exert antiatherogenic action by inhibition the production of monocyte inflammatory cytokines, inhibition of expression of adhesion molecules in endothelial cells, inhibition of the proliferation of vascular smooth muscle cells and have antioxidative effects. The United Kingdom Prospective Diabetes Study (UKPDS), published in 1998, found that the use of sulphonylureas had no increase in cardiovascular mortality and that metformin therapy in obese individuals with type 2 diabetes mellitus was associated with reduced cardiovascular death. Recently, the STOP-NIDDM trial has been shown that patients with impaired glucose tolerance treated with the alpha-glucosidase inhibitor acarbose had a significant reduction in the risk of cardiovascular disease. Currently, the results of the UKPDS trial are the only available clinical data on which to base the choice of treatment for type 2 diabetic patients. When a glucose-lowering oral drug is considered necessary and is not contraindicated, the firstline choice is a sulphonylurea or a glinide (repaglinide or nateglinide) for diabetics who are not overweight and metformin for those who are.

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“…Ciglitazone, the prototype from this class, was found to reduce hyperglycemia, hyperlipidemia, and hypertriglyceridemia in insulin-resistant animal models, but not in normoglycemic animals (Fujita et al, 1983;Chang et al, 1983). Ciglitazone was, therefore, taken for human trials but was withdrawn later because of low potency and the appearance of cataracts in animals receiving this drug for longer period of time.…”

Section: Introductionmentioning

confidence: 99%

Novel glitazones: glucose uptake and cytotoxic activities, and structure–activity relationships

Kumar

Patel

et al. 2011

Med Chem Res

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In this article, two series of novel glitazones are reported for their synthesis, in vitro glucose uptake activity by the rat hemi-diaphragm, and in vitro cytotoxic activity against human carcinoma HEp-2 (epidermoid carcinoma of the larynx) and A549 (human lung cancer cell line) cells. Some of the compounds exhibit good glucose uptake and cytotoxic activities. Compound 5 with 2,4-dichlorophenol moiety connected to TZD via the two carbon linker has exhibited good glucose uptake activity. One of the compounds exhibits both cytotoxic and glucose uptake activities (compound 4). Illustrations about their synthesis, and in vitro glucose uptake and cytotoxic activities are described along with their structure-activity relationships.

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Reduction of insulin resistance in obese and/or diabetic animals by 5-[4-(1-methylcyclohexylmethoxy)benzyl]-thiazolidine-2,4-dione (ADD-3878, U-63,287, ciglitazone), a new antidiabetic agent

Cited by 123 publications

References 0 publications

Effect of thiazolidinediones on bile acid transport in rat liver

Effect of thiazolidinediones on bile acid transport in rat liver

Kardiovaskul�re Effekte oraler Antidiabetika

Novel glitazones: glucose uptake and cytotoxic activities, and structure–activity relationships

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