Further studies on ethyl 5-hydroxy-indole-3-carboxylate scaffold: Design, synthesis and evaluation of 2-phenylthiomethyl-indole derivatives as efficient inhibitors of human 5-lipoxygenase

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Further studies on ethyl 5-hydroxy-indole-3-carboxylate scaffold: Design, synthesis and evaluation of 2-phenylthiomethyl-indole derivatives as efficient inhibitors of human 5-lipoxygenase

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作者：Antonella Peduto^a ; ^f ; Ferdinando Bruno^b ; Friedrike Dehm^c ; Verena Krauth^c ; Paolo de Caprariis^b ; Christina Weinigel^d ; Dagmar Barz^d ; Antonio Massa^e ; Mario De Rosa^a ; Oliver Werz^c ; Rosanna Filosa^a ; ^{rosanna.filosa@unina2.it" class="auth_mail}
关键词：5-Lipoxygenase ; Leukotriene ; Indoles
刊名：European Journal of Medicinal Chemistry
出版年：23 June 2014
年：2014
卷：81
期：Complete
页码：492-498
全文大小：610 K

文摘

•: We described SAR analysis of novel series of ethyl 5-hydroxyindole-3-carboxylate.
•: We examined changes in positioning of the substituents at the phenylthiomethyl ring.
•: We studied the inhibitory activities on 5-LO product synthesis.
•: We determined the inhibitory activities of the major AA-metabolizing enzymes with the most active derivative.

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