1903-65-7Relevant academic research and scientific papers
Design, synthesis, and progress toward optimization of potent small molecule antagonists of CC chemokine receptor 8 (CCR8)
Ghosh, Shomir,Elder, Amy,Guo, Jianping,Mani, Ukti,Patane, Michael,Carson, Kenneth,Ye, Qing,Bennett, Robert,Chi, Shannon,Jenkins, Tracy,Guan, Bing,Kolbeck, Roland,Smith, Sean,Zhang, Cheng,LaRosa, Gregory,Jaffee, Bruce,Yang, Hua,Eddy, Priya,Lu, Chuang,Uttamsingh, Vinita,Horlick, Robert,Harriman, Geraldine,Flynn, Daniel
, p. 2669 - 2672 (2007/10/03)
Activation of CCR8 by its ligand CCL1 may play an important role in diseases such as asthma, multiple sclerosis, and cancer. The study of small molecule CCR8 antagonists will help establish the validation of these hypotheses. We report the design, synthesis, and progress toward optimization of potent small molecule CCR8 antagonists identified from a high-throughput screen. These analogues exhibit good potency in binding and chemotaxis assays, show good selectivity versus the hERG channel, and have good eADME (early absorption, distribution, metabolism, and excretion) profiles.
Facile Reduction of Pyridines with Nickel-Aluminum Alloy
Lunn, George,Sansone, Eric B.
, p. 513 - 517 (2007/10/02)
Nickel-aluminum alloy in dilute base can be used to reduce a variety of pyridines, quinolines, and isoquinoline to the corresponding piperidines, 1,2,3,4-tetrahydroquinolines, and 1,2,3,4-tetrahydroisoquinoline in good yield.The reaction is simple to perform, and high temperatures, high pressures, or hydrogen atmospheres are not required.The reaction is accelerated by substituents in the 2-position and by electron-withdrawing groups in the 3- and 4-positions while electron-supplying groups in the 3- and 4-positions retard the reaction.The major product isolated from the reduction of 2-phenylpyridine was 2-cyclohexylpiperidine hydrochloride.With isoniazid (1) and iproniazid (4) the pyridine ring is hydrogenated before the hydrazine is cleaved.
