Indanes--Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors.
Med Res Rev
; 35(6): 1097-126, 2015 Nov.
Article
em En
| MEDLINE
| ID: mdl-26018667
ABSTRACT
The indane (2,3-dihydro-1H-indene) ring system is an attractive scaffold for biologically active compounds due to the combination of aromatic and aliphatic properties fused together in one rigid system. This bicyclic structure provides a wide range of possibilities to incorporate specific substituents in different directionalities, thus being an attractive scaffold for medicinal chemists. Notably, many indane-based compounds are being used in the clinic to treat various diseases, such as indinavir, an HIV-1 protease inhibitor; indantadol, a potent Monoamine Oxidase (MAO)-inhibitor; the amine uptake inhibitor indatraline; and the ultra-long-acting ß-adrenoceptor agonist indacaterol. Given the diversity of targets these drugs act on, one could argue that the indane ring system is a privileged substructure. In the present review, the synthetic and medicinal chemistry of the indane ring system is described. In more detail, it contains a comprehensive overview of compounds bearing the indane substructure with G protein coupled receptor (GPCR) activity, with particular emphasis on their structure-activity relationships (SAR).
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Base de dados:
MEDLINE
Assunto principal:
Receptores Acoplados a Proteínas G
/
Indanos
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article