Ken-ichi Fujimura

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We studied the synthetic modification of structurally similar N-mercaptoacyl-L-proline and (4R)-N-mercaptoacylthiazolidine-4-carboxylic acid to obtain potent leukotriene A(4) (LTA(4)) hydrolase inhibitors. An N-mercaptoacyl group, (2S)-3-mercapto-2-methylpropionyl group, was effective for both scaffolds. Additional introduction of a large substituent such(More)
US, a phase III clinical study is currently underway. Hydrolyzed to its corresponding active acid form (AFP-172; 3) after topical application, compound 1 exhibits strong IOP reducing effects by increasing the drainage of aqueous humor through the uveoscleral outflow route. Compound 3 has a stronger binding affinity (Ki=0.4 nm) [4] for the PGF2a receptor(More)
We studied synthetic modifications of N-mercaptoacylamino acid derivatives to develop a new class of leukotriene A(4) (LTA(4)) hydrolase inhibitors. S-(4-Dimethylamino)benzyl-l-cysteine derivative 2a (SA6541) showed inhibitory activity against LTA(4) hydrolase (IC(50), 270nM) and selectivity over other metallopeptidases except angiotensin-converting enzyme(More)
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