13314-69-7Relevant articles and documents
Substituted piperidines - Highly potent renin inhibitors due to induced fit adaptation of tile active site
Vieira, Eric,Binggeli, Alfred,Breu, Volker,Bur, Daniel,Fischli, Walter,Gueller, Rolf,Hirth, Georges,Maerki, Hans Peter,Mueller, Marcel,Oefner, Christian,Scalone, Michelangelo,Stadler, Heinz,Wilhelm, Maurice,Wostl, Wolfgang
, p. 1397 - 1402 (1999)
The identification, synthesis and activity of a novel class of piperidine renin inhibitors is presented. The most active compounds show activities in the picomolar range and are among the most potent renin inhibitors ever identified.
BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder
Marcin, Lawrence R.,Warrier, Jayakumar,Thangathirupathy, Srinivasan,Shi, Jianliang,Karageorge, George N.,Pearce, Bradley C.,Ng, Alicia,Park, Hyunsoo,Kempson, James,Li, Jianqing,Zhang, Huiping,Mathur, Arvind,Reddy, Aliphedi B.,Nagaraju,Tonukunuru, Gopikishan,Gupta, Grandhi V. R. K. M.,Kamble, Manjunatha,Mannoori, Raju,Cheruku, Srinivas,Jogi, Srinivas,Gulia, Jyoti,Bastia, Tanmaya,Sanmathi, Charulatha,Aher, Jayant,Kallem, Rajareddy,Srikumar, Bettadapura N.,Vijaya, Kumar Kuchibhotla,Naidu, Pattipati S.,Paschapur, Mahesh,Kalidindi, Narasimharaju,Vikramadithyan, Reeba,Ramarao, Manjunath,Denton, Rex,Molski, Thaddeus,Shields, Eric,Subramanian, Murali,Zhuo, Xiaoliang,Nophsker, Michelle,Simmermacher, Jean,Sinz, Michael,Albright, Charlie,Bristow, Linda J.,Islam, Imadul,Bronson, Joanne J.,Olson, Richard E.,King, Dalton,Thompson, Lorin A.,Macor, John E.
, p. 472 - 477 (2018/05/23)
There is a significant unmet medical need for more efficacious and rapidly acting antidepressants. Toward this end, negative allosteric modulators of the N-methyl-d-aspartate receptor subtype GluN2B have demonstrated encouraging therapeutic potential. We
Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6- tetrahydropyridines as 5-HT2C agonists
Conway, Richard J.,Valant, Celine,Christopoulos, Arthur,Robertson, Alan D.,Capuano, Ben,Crosby, Ian T.
, p. 2560 - 2564 (2012/05/05)
A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the 5-HT2C receptor studied to determine whether either series showed noteworthy agonist activity. Structure-activity relationships were developed from the performed receptor binding assays and functional studies, and the results of the analysis are presented herein.