194996-03-7Relevant articles and documents
Synthesis and evaluation of (4-chlorobenzhydryl) piperazine amides as sodium channel Nav1.7 inhibitors
Back, Seung Keun,Kam, Yoo Lim,Oh, Jung Ae,Na, Heung Sik,Ih, Uhtaek,Park Choo, Hea-Young
, p. 2290 - 2297 (2015/09/22)
Blockage of voltage-gated sodium channels is used to treat neuropathic pain which is chronic and can become debilitating. Sodium channels Nav1.7-1.9 are especially attractive targets for drug discovery because of the broad therapeutic potential of their m
Solution-phase combinatorial synthesis of nonpeptide bradykinin antagonists
Kam, Yoo Lim,Rhee, Soo-Jin,Choo, Hea-Young P.
, p. 3543 - 3552 (2007/10/03)
We describe the solution-phase combinatorial synthesis and pharmacological effect of fifty N,N′-substituted-N″-1-(4- chlorobenzhydryl)piperazine iminodiacetic acid triamide derivatives as nonpeptide B2 antagonists. The synthesized compounds wer
Higher order iminodiacetic acid libraries for probing protein-protein interactions
Boger, Dale L.,Goldberg, Joel,Jiang, Weiqin,Chai, Wenying,Ducray, Pierre,Lee, Jae Kyoo,Ozer, Rachel S.,Andersson, Carl-Magnus
, p. 1347 - 1378 (2007/10/03)
Full details of the preparation of iminodiacetic acid diamide dimer (2040 compounds), trimer (560 compounds), and tetramer (1596 compounds) libraries by multistep convergent solution-phase synthesis for studying protein-protein interactions are provided. The libraries were assembled in a format providing small 8-10 compound mixtures and the deconvolution of many of the small mixtures to identify screening leads by resynthesis of the individual components have been conducted for 320 of the individual compounds to date. A representative example of the subsequent exploration of the structure-activity relationships for an identified receptor binding antagonist (200 additional individual compounds) and steps taken for potential elaboration to a receptor dimerization agonist are defined with preparation of representative linked dimers (70 compounds). Copyright (C) 1998 Elsevier Science Ltd.