27958-97-0Relevant articles and documents
Synthesis and antimalarial activity of new analogues of amodiaquine
Delarue-Cochin, Sandrine,Paunescu, Emilia,Maes, Louis,Mouray, Elisabeth,Sergheraert, Christian,Grellier, Philippe,Melnyk, Patricia
, p. 252 - 260 (2008/09/18)
In order to determine the real significance of the 4′-phenolic group in the antimalarial activity and/or cytotoxicity of amodiaquine (AQ), analogues for which this functionality was shifted or modified were synthesized. Good in vitro antimalarial activity
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase
Zhao, Guohua,Bolton, Scott A.,Kwon, Chet,Hartl, Karen S.,Seiler, Steven M.,Slusarchyk, William A.,Sutton, James C.,Bisacchi, Gregory S.
, p. 309 - 312 (2007/10/03)
The serine protease tryptase has been associated with a broad range of allergic and inflammatory diseases and, in particular, has been implicated as a critical mediator of asthma. The inhibition of tryptase therefore has the potential to be a valuable therapy for asthma. The synthesis, employing solution phase parallel methods, and SAR of a series of novel 2-azepanone tryptase inhibitors are presented. A member of this series, 8t, was identified as a potent inhibitor of human tryptase (IC50=38 nM) with selectivity ≤330-fold versus related serine proteases (trypsin, plasmin, uPA, tPA, APC, alpha-thrombin, and FXa).