1070749-80-2Relevant academic research and scientific papers
Function-regulating pharmacophores in a sulfonamide class of glucocorticoid receptor agonists
Kuzmich, Daniel,Bentzien, Joerg,Betageri, Raj,Disalvo, Darren,Fadra-Khan, Tazmeen,Harcken, Christian,Kukulka, Alison,Nabozny, Gerald,Nelson, Richard,Pack, Edward,Souza, Donald,Thomson, David
, p. 6640 - 6644 (2014/01/06)
A class of α-methyltryptamine sulfonamide glucocorticoid receptor (GR) modulators was optimized for agonist activity. The design of ligands was aided by molecular modeling, and key function-regulating pharmacophoric points were identified that are critical in achieving the desired agonist effect in cell based assays. Compound 27 was profiled in vitro and in vivo in models of inflammation. Analogs could be rapidly prepared in a parallel approach from aziridine building blocks.
GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
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, (2008/12/04)
Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, X, R7, and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
