Targeting Peroxisome Proliferator-Activated Receptors Using Thiazolidinediones: Strategy for Design of Novel Antidiabetic Drugs

Table 1

Pharmacological and chemical classification of PPARγ agonists.

(I) Strong/full PPARγ agonists
(1) Endogenous ligands:	9-HODE, 13-HODE, 15-deoxy-^12,14-prostaglandin J2,; Prostaglandin PGJ2
(2) Natural ligands of plant origin:
(a) Unsaturated fatty acids and hydroxy unsaturated fatty acids
(b) Flavonoids:	Luteolin, Quercetin, Kaempferol, (-) Catechin; 2-hydroxychalcone, Biochanin A, Genistein,; 6-hydroxydaidzein
(c) Stilbenes:	Resveratrol, Amorphastilbol
(d) Amorfrutins:	Amorfrutin 1, Amorfrutin 2, Amorfrutin 3
(e) Polyacetylenes:	Falcarindiol
(f) Sesquiterpene lactones:	Deoxyelephantopin
(g) Diterpene quinone derivatives:	Sargaquinoic acid, Sargahydroquinoic acid
(3) Synthetic strong PPARγ agonists:
(a) Thiazolidinediones or Glitazones:	Rosiglitazone, Pioglitazone, Troglitazone, Ciglitazone Rivoglitazone, Englitazone
(b) Non-thiazolidinediones:
(i) L-tyrosine analogue:	Farglitazar
(ii) Sulfonamide derivative:	INT 131
(II) Selective/partial PPARγ agonists
(1) Thiazolidinediones:	Balaglitazone
(2) Benzodiazole derivative:	Telmisartan
(III) DUAL PPARα/γ AGONISTS
(1) Thiazolidinediones:	Netoglitazone, experimental compounds KRP 297,; MK 767, DRF 2189
(2) Glitazars or non-thiazolidinediones	Muraglitazar, Tesaglitazar, Navaglitazar, Ragaglitazar Aleglitazar
(IV) PPAR panagonists (agonists of PPARα/β/γ subtypes)
(1) Fibrate drug	Benzafibrate
(2) Miscellaneous, non-thiazolidinedione derivative	Chiglitazar
(3) Fibric acid derivative	Experimental compound ZBH201102
(4) Thiazole derivative	GW-677954
(5) Oxazole derivative	LY-465608
(V) SPPARγM (selective PPARγ modulator); (Phenylacetic acid derivative)	Metaglidasen
(VI) NOVEL PPARγ/FFAR1 DUAL AGONISTS
(1) Thiazolidinediones	Experimental compounds KM-1, KM-2, KM-5

Compounds have been withdrawn from market or discontinued from clinical trials.