Synthesis and biological evaluation of N-mercaptoacylcysteine derivatives as leukotriene A4 hydrolase inhibitors
We studied synthetic modifications of N-mercaptoacylamino acid derivatives to develop a new class of leukotriene A4 (LTA4) hydrolase inhibitors. S-(4-Dimethylamino)benzyl-l-cysteine derivative 2a (SA6541) showed inhibitory activity against LTA4 hydrolase (IC50, 270 nM) and selectivity over other metallopeptidases except angiotensin-converting enzyme (ACE, IC50, 520 nM). Modification at the para-substituent of the phenyl ring of compound 2a improved LTA4 hydrolase inhibitory activity as well as selectivity over ACE. Finally, we obtained S-(4-cyclohexyl)benzy-l-cysteine derivatives 11l and 16i as potent and selective LTA4 hydrolase inhibitors.
PCT No. PCT/JP97/03124 Sec. 371 Date Mar. 1, 1999 Sec. 102(e) Date Mar. 1, 1999 PCT Filed Sep. 5, 1997 PCT Pub. No. WO98/09943 PCT Pub. Date May 12, 1998A sulfur-containing amino acid compound having a high inhibitory activity on LTA4 hydrolase which is r
-
(2008/06/13)
More Articles about upstream products of 204695-04-5