N-Benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors

…, J Litchfield, M Makowski, K Martin, TJ McLellan…

文献索引：Atkinson, Karen A.; Beretta, Elena E.; Brown, Janice A.; Castrodad, Mayda; Chen, Yue; Cosgrove, Judith M.; Du, Ping; Litchfield, John; Makowski, Michael; Martin, Kelly; McLellan, Thomas J.; Neagu, Constantin; Perry, David A.; Piotrowski, David W.; Steppan, Claire M.; Trilles, Richard Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 6 p. 1621 - 1625

全文：HTML全文

被引用次数: 21

摘要

A potent, small molecule inhibitor with a favorable pharmacokinetic profile to allow for sustained SCD inhibition in vivo was identified. Starting from a low MW acyl guanidine (5a), identified with a RapidFire High-Throughput Mass Spectrometry (RF-MS) assay, iterative library design was used to rapidly probe the amide and tail regions of the molecule. Singleton synthesis was used to probe core changes. Biological evaluation of a SCD ...