480423-60-7Relevant articles and documents
Discovery of new C3aR ligands. Part 1: Arginine derivatives
Denonne, Frederic,Binet, Sophie,Burton, Maggi,Collart, Philippe,Dipesa, Alan,Ganguly, Tanmoy,Giannaras, Alexander,Kumar, Seema,Lewis, Timothy,Maounis, Florence,Nicolas, Jean-Marie,Mansley, Tamsin,Pasau, Patrick,Preda, Dorin,Stebbins, Karin,Volosov, Alexander,Zou, Dong
, p. 3258 - 3261 (2008/02/08)
The synthesis and in vitro binding of several new arginine-containing C3aR ligands are reported. DMPK properties and functional activities of selected compounds have been evaluated. One compound is shown to be active in an in vivo model of airway inflamma
(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1
Lee, Sunkyung,Yi, Kyu Yang,Hwang, Sun Kyung,Lee, Byung Ho,Yoo, Sung-Eun,Lee, Kyunghee
, p. 2882 - 2891 (2007/10/03)
A series of (5-arylfuran-2-ylcarbonyl)guanidines was synthesized and evaluated for the NHE-1 inhibitory activity and cardiprotective efficacy against ischemia-reperfusion injury. Starting with (5-phenylfuran-2-ylcarbonyl) guanidine 47 with a moderate inhibitory effect on NHE-1, the compounds with various substituents at the phenyl ring were investigated with the aim to optimize the potency. In this study, the 2,5-disubstituted compounds appeared to have better activities than the other analogues, and the 2-methoxy-5- chlorophenyl compound 85 was found as a potent inhibitor of NHE-1 (IC 50 = 0.081 μM). Furthermore, 85 showed a marked reduction of infarct size in the rat myocardial infarction model in vivo and significant improvement of cardiac contractile function in the isolated rat heart ischemia model in vitro.
