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    J Med Chem. 2010 Sep 23;53(18):6681-98.

    Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics.

    Riether D, Harcken C, Razavi H, Kuzmich D, Gilmore T, Bentzien J, Pack EJ, Souza D, Nelson RM, Kukulka A, Fadra TN, Zuvela-Jelaska L, Pelletier J, Dinallo R, Panzenbeck M, Torcellini C, Nabozny GH, Thomson DS.

    Source

    Department of Medicinal Chemistry, Department of Immunology and Inflammation, and Drug Discovery Support, Boehringer-Ingelheim Pharmaceuticals Inc., 900 Ridgebury Road, Ridgefield, Connecticut 06877, USA. doris.riether@boehringer-ingelheim.com

    Abstract

    Syntheses and structure-activity relationships (SAR) of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain azaindole moieties as A-ring mimetics and display various degrees of in vitro dissociation between gene transrepression and transactivation. Collagen induced arthritis studies in mouse have demonstrated that in vitro dissociated compounds (R)-16 and (R)-37 have steroid-like anti-inflammatory properties with improved metabolic side effect profiles, such as a reduced increase in body fat and serum insulin levels, compared to steroids.

    PMID:
    20735001
    [PubMed - indexed for MEDLINE]

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