1361190-12-6Relevant articles and documents
Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: Discovery of 2-[4-(3-{(R)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]- N, N -dimethyl-acetamide (BI 665915)
Takahashi, Hidenori,Riether, Doris,Bartolozzi, Alessandra,Bosanac, Todd,Berger, Valentina,Binetti, Ralph,Broadwater, John,Chen, Zhidong,Crux, Rebecca,De Lombaert, Stéphane,Dave, Rajvee,Dines, Jonathon A.,Fadra-Khan, Tazmeen,Flegg, Adam,Garrigou, Michael,Hao, Ming-Hong,Huber, John,Hutzler, J. Matthew,Kerr, Steven,Kotey, Adrian,Liu, Weimin,Lo, Ho Yin,Loke, Pui Leng,Mahaney, Paige E.,Morwick, Tina M.,Napier, Spencer,Olague, Alan,Pack, Edward,Padyana, Anil K.,Thomson, David S.,Tye, Heather,Wu, Lifen,Zindell, Renee M.,Abeywardane, Asitha,Simpson, Thomas
, p. 1669 - 1690 (2015/04/21)
The synthesis, structure-activity relationship (SAR), and evolution of a novel series of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitors are described. The use of structure-guided drug design techniques provided compounds that demonstrated excellent FLAP binding potency (IC50 4 synthesis in human whole blood (IC50 4 production.
