- Synthesis and antimalarial activity of new analogues of amodiaquine
-
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
- Delarue-Cochin, Sandrine,Paunescu, Emilia,Maes, Louis,Mouray, Elisabeth,Sergheraert, Christian,Grellier, Philippe,Melnyk, Patricia
-
p. 252 - 260
(2008/09/18)
-
- PYRIMIDINE UREA DERIVATIVES AS KINASE INHIBITORS
-
The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
- -
-
Page/Page column 279
(2008/06/13)
-
- Synthesis of potent and selective 2-azepanone inhibitors of human tryptase
-
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).
- 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)
-
