83527-99-5Relevant articles and documents
Synthesis and biological evaluation of biphenyl amides that modulate the US28 receptor
Kralj, Ana,Kurt, Elif,Tschammer, Nuska,Heinrich, Markus R.
, p. 151 - 168 (2014/01/17)
To prepare and biologically evaluate 38 new potential US28 allosteric modulators, we employed a straightforward synthetic route involving radical arylation. The study was based on a former lead structure but with the dihydroisoquinolinone moiety replaced by substituted biphenyls. The investigation of structure-activity relationships among the new biphenyl-derived ligands led to a preliminary pharmacophore model and the discovery of four promising candidates with full inverse agonist properties. Hit HCMV GPCRs ASAP! Employing a straightforward synthetic access involving radical arylation, 38 new potential US28 allosteric modulators were prepared and biologically evaluated. The investigation of structure-activity relationships among the new biphenyl-derived ligands led to a consistent model and the discovery of four promising candidates with full inverse agonist properties. Copyright
Facile synthesis of biologically active heterocycles by indium-induced reactions of aromatic nitro compounds in aqueous ethanol
Banik, Bimal K.,Banik, Indrani,Samajdar, Susanta,Wilson, Mary
, p. 283 - 296 (2007/10/03)
Indium/ammonium chloride-induced reduction of aromatic nitro compounds to aromatic amines in aqueous ethanol was developed. Useful chemoselectivity was observed in the reduction reaction. This method was extended to reductive cyclization and rearrangement toward the synthesis of various biologically active heterocycles, including quinoline, oxazines, quinalonones, and phenanthridine in excellent yield. The oxophilicity of indium metal influenced the reaction in aqueous ethanol. Metals like zinc and tin were not effective in promoting this kind of reactions under the present environmentally friendly conditions.
STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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, (2008/06/13)
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.