149489-22-5Relevant academic research and scientific papers
Discovery of Highly Potent Liver X Receptor β Agonists
Kick, Ellen K.,Busch, Brett B.,Martin, Richard,Stevens, William C.,Bollu, Venkataiah,Xie, Yinong,Boren, Brant C.,Nyman, Michael C.,Nanao, Max H.,Nguyen, Lam,Plonowski, Artur,Schulman, Ira G.,Yan, Grace,Zhang, Huiping,Hou, Xiaoping,Valente, Meriah N.,Narayanan, Rangaraj,Behnia, Kamelia,Rodrigues, A. David,Brock, Barry,Smalley, James,Cantor, Glenn H.,Lupisella, John,Sleph, Paul,Grimm, Denise,Ostrowski, Jacek,Wexler, Ruth R.,Kirchgessner, Todd,Mohan, Raju
supporting information, p. 1207 - 1212 (2016/12/18)
Introducing a uniquely substituted phenyl sulfone into a series of biphenyl imidazole liver X receptor (LXR) agonists afforded a dramatic potency improvement for induction of ATP binding cassette transporters, ABCA1 and ABCG1, in human whole blood. The ag
Structure-activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors
Teng, Xin,Keys, Heather,Jeevanandam, Arumugasamy,Porco Jr., John A.,Degterev, Alexei,Yuan, Junying,Cuny, Gregory D.
, p. 6836 - 6840 (2008/03/14)
Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling non-regulated necrosis. This form of cell death can be induced in an array of cell types in apoptotic deficient conditions with death receptor family ligands. A series of [1,2,3]thiadiazole benzylamides was found to be potent necroptosis inhibitors (called necrostatins). A structure-activity relationship study revealed that small cyclic alkyl groups (i.e. cyclopropyl) and 2,6-dihalobenzylamides at the 4- and 5-positions of the [1,2,3]thiadiazole, respectively, were optimal. In addition, when a small alkyl group (i.e. methyl) was present on the benzylic position all the necroptosis inhibitory activity resided with the (S)-enantiomer. Finally, replacement of the [1,2,3]thiadiazole with a variety of thiophene derivatives was tolerated, although some erosion of potency was observed.
Method for inhibition of HIV related viruses
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, (2008/06/13)
Treatment of AIDS, inhibition of the replication of HIV and related viruses thereof, and formulations using thiourea derivative compounds or salts thereof is disclosed. Also disclosed are novel thiourea derivative compounds.
