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

Autor:	Josephine Pelletier, Jörg Bentzien, Doris Riether, Richard M. Nelson, David S. Thomson, Tazmeen N. Fadra, Roger M. Dinallo, Daniel Kuzmich, Gerald Nabozny, Donald Souza, Alison Kukulka, Ljiljana Zuvela-Jelaska, Gilmore Thomas A, Mark Panzenbeck, Edward Pack, Christian Harcken, Carol A. Torcellini, Hossein Razavi
Rok vydání:	2010
Předmět:	Models Molecular Transcriptional Activation medicine.medical_specialty Pyridines medicine.medical_treatment Serum insulin Biological Availability Pharmacology Steroid Rats Sprague-Dawley Transactivation chemistry.chemical_compound Mice Structure-Activity Relationship Glucocorticoid receptor Aromatase Receptors Glucocorticoid Internal medicine Drug Discovery medicine Animals Humans Insulin Pyrroles Cells Cultured Transrepression Mice Inbred BALB C Nonsteroidal Aromatase Inhibitors Interleukin-6 Anti-Inflammatory Agents Non-Steroidal Hydrogen Bonding Stereoisomerism Arthritis Experimental In vitro Rats Endocrinology chemistry Adipose Tissue Enzyme Induction Molecular Medicine Female Steroids Glucocorticoid medicine.drug Interleukin-1
Zdroj:	Journal of medicinal chemistry. 53(18)
ISSN:	1520-4804
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ffc2413c5f4218a8c1f3ea1d2613039 https://pubmed.ncbi.nlm.nih.gov/20735001 Zobrazit plný text záznamu