Thiazolidinediones and PPAR orchestra as antidiabetic agents: From past to present

Dec 19, 2016European journal of medicinal chemistry

Thiazolidinediones and PPARs as diabetes medicines: Their role from past to present

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Abstract

Thiazolidinediones (TZDs) have undergone significant chemical modifications over the past two decades to enhance their effectiveness as antidiabetic agents.

TZDs were the first class of drugs identified as modulators of PPARγ, which is crucial in the management of type 2 diabetes.
Initial research focused on the hypoglycemic and hypolipidemic effects of TZDs.
Chemical modifications of TZDs, particularly in the linker region, have evolved from oxymethyl to oxyethyl and oxyethylamino structures.
Comparative studies often reported both benzyl and benzylidene derivatives to assess their relative efficacy.
Recent efforts have aimed to restrict the flexibility of the linker by introducing cyclic structures.

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Thiazolidinediones a class of drug, that provided a major breakthrough in the management of type 2 diabetes since 1990. Following the discovery of PPARs, TZDs were the first class to be reported as PPARγ modulators. This review is an attempt to summarize the chemical modifications around TZDs in past two decades to obtain a potent antidiabetic molecule. TZDs literature were initially dominated by their hypoglycemic & hypolipidemic activities, later PPARγ activity was also been incorporated. Moreover, in some cases, both benzyl and benzylidene derivatives were reported in the same manuscript for the sake of comparison. We thought of presenting the review on the basis of the variation in the linker region. Optimal linker at the time of discovery of the Ciglitazone was oxymethyl and it went on to evolve as oxyethyl (Pioglitazone) and oxyethylamino (Rosiglitazone). Few attempts were made to restrict the flexibility of the linker by introducing the cyclic structures and were summarized immediately after the respective linker class.

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Thiazolidinediones and PPAR orchestra as antidiabetic agents: From past to present

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