38289-22-4Relevant articles and documents
Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV
Namoto, Kenji,Sirockin, Finton,Ostermann, Nils,Gessier, Francois,Flohr, Stefanie,Sedrani, Richard,Gerhartz, Bernd,Trappe, J?rg,Hassiepen, Ulrich,Duttaroy, Alokesh,Ferreira, Suzie,Sutton, Jon M.,Clark, David E.,Fenton, Garry,Beswick, Mandy,Baeschlin, Daniel K.
, p. 731 - 736 (2014/02/14)
The successful launches of dipeptidyl peptidase IV (DPP IV) inhibitors as oral anti-diabetics warrant and spur the further quest for additional chemical entities in this promising class of therapeutics. Numerous pharmaceutical companies have pursued their proprietary candidates towards the clinic, resulting in a large body of published chemical structures associated with DPP IV. Herein, we report the discovery of a novel chemotype for DPP IV inhibition based on the C-(1-aryl-cyclohexyl)-methylamine scaffold and its optimization to compounds which selectively inhibit DPP IV at low-nM potency and exhibit an excellent oral pharmacokinetic profile in the rat. 2014 Elsevier Ltd. All rights reserved.
Benzamide derivatives as blockers of Kv1.3 ion channel
Miao, Shouwu,Bao, Jianming,Garcia, Maria L.,Goulet, Joung L.,Hong, Xingfang J.,Kaczorowski, Gregory J.,Kayser, Frank,Koo, Gloria C.,Kotliar, Andrew,Schmalhofer, William A.,Shah, Kashmira,Sinclair, Peter J.,Slaughter, Robert S.,Springer, Marty S.,Staruch, Mary Jo,Tsou, Nancy N.,Wong, Frederick,Parsons, William H.,Rupprecht, Kathleen M.
, p. 1161 - 1164 (2007/10/03)
The voltage-gated potassium channel, Kv1.3, is present in human T-lymphocytes. Blockade of Kv1.3 results in T-cell depolarization, inhibition of T-cell activation, and attenuation of immune responses in vivo. A class of benzamide Kv1.3 channel inhibitors
