Discovery and Optimization of N-Acyl-6-sulfonamide-tetrahydroquinoline Derivatives as Novel Non-Steroidal Selective Glucocorticoid Receptor Modulators.
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DOI: 10.1021/acs.jmedchem.2c01082
Abstract: Selective glucocorticoid receptor modulators (SGRMs), which can dissociate the transactivation from the transrepression of the glucocorticoid receptor (GR), are regarded as very promising therapeutics for inflammatory and autoimmune diseases. We previously discovered a SGRM HP-19… read more here.
Keywords: glucocorticoid; receptor modulators; glucocorticoid receptor; acyl sulfonamide ... See more keywords
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain.
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DOI: 10.1021/acs.jmedchem.7b01826
Abstract: The sodium channel NaV1.7 has emerged as a promising target for the treatment of pain based on strong genetic validation of its role in nociception. In recent years, a number of aryl and acyl sulfonamides… read more here.
Keywords: acyl sulfonamide; triazolo pyridin; treatment pain;