Bioorganic & Medicinal Chemistry Letters 1984-01-01

Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.

C Jakobs, L Sweetman, W L Nyhan, S Packman

Index: Bioorg. Med. Chem. Lett. 15(22) , 5035-8, (2005)

Full Text: HTML

Abstract

A series of novel aryl indole-2-carboxylic acids has been identified as potent selective PPARgamma modulators. Their chemical synthesis and in vitro activities are discussed. Compound 5 was selected for in vivo testing in the db/db mouse model of type 2 diabetes and resulted in reduction of hyperglycemia at comparable plasma exposure when compared to rosiglitazone.

Related Compounds

  • Indole-2-carboxyli...

Related Articles:

Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.

2009-07-15

[Bioorg. Med. Chem. 17 , 5219-28, (2009)]

In vitro and in vivo assessment of the antioxidant activity of melatonin and related indole derivatives.

2002-06-01

[Gen. Physiol. Biophys. 21(2) , 153-62, (2002)]

Protonated carbonic acid and reactive intermediates in the acidic decarboxylation of indolecarboxylic acids.

2012-08-03

[J. Org. Chem. 77(15) , 6505-9, (2012)]

Formation of indigo and related compounds from indolecarboxylic acids by aromatic acid-degrading bacteria: chromogenic reactions for cloning genes encoding dioxygenases that act on aromatic acids.

1995-12-01

[J. Bacteriol. 177(23) , 6983-8, (1995)]

Assembly of indole-2-carboxylic acid esters through a ligand-free copper-catalysed cascade process.

2009-12-28

[Chem. Commun. (Camb.) (48) , 7581-3, (2009)]

More Articles...