607715-32-2Relevant academic research and scientific papers
(±)-2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinolines as a new class of specific bradycardic agents
Kubota, Hideki,Kakefuda, Akio,Watanabe, Toshihiro,Taguchi, Yasuko,Ishii, Noe,Masuda, Noriyuki,Sakamoto, Shuichi,Tsukamoto, Shin-Ichi
, p. 2155 - 2158 (2003)
A series of (±)-2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinolines were prepared and their bradycardic activities were examined in isolated guinea-pigs' right atria and in anesthetized rats. Modifications on the benzyl moiety of the parent compound, 1, led to the identification of compound 11e as a potent and specific bradycardic agent.
Structure-activity relationships of the peptide deformylase inhibitor BB-3497: Modification of the methylene spacer and the P1′ side chain
Davies, Stephen J.,Ayscough, Andrew P.,Beckett, R. Paul,Bragg, Ryan A.,Clements, John M.,Doel, Sheila,Grew, Christine,Launchbury, Steven B.,Perkins, Gemma M.,Pratt, Lisa M.,Smith, Helen K.,Spavold, Zoe M.,Thomas, S. Wayne,Todd, Richard S.,Whittaker, Mark
, p. 2709 - 2713 (2007/10/03)
Structural modifications to the peptide deformylase inhibitor BB-3497 are described. In this paper, we describe the initial SAR around this lead for modifications to the methylene spacer and the P1′ side chain. Enzyme inhibition and antibacterial activity data revealed that the optimum distance between the N-formyl hydroxylamine metal binding group and the P1′ side chain is one unsubstituted methylene unit. Additionally, lipophilic P1′ side chains that closely mimic the methionine residue in the substrate provided compounds with the best microbiological profile.
