Identification of novel benzimidazole derivatives as inhibitors of leukotriene biosynthesis by virtual screening targeting 5-lipoxygenase-activating protein (FLAP)

…, W Altenhofen, C Weinigel, D Barz, J Gerstmeier…

Index: Banoglu, Erden; Caliskan, Burcu; Luderer, Susann; Eren, Goekcen; Oezkan, Yagmur; Altenhofen, Wolfram; Weinigel, Christina; Barz, Dagmar; Gerstmeier, Jana; Pergola, Carlo; Werz, Oliver Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 12 p. 3728 - 3741

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Citation Number: 17

Abstract

Pharmacological suppression of leukotriene biosynthesis by 5-lipoxygenase (5-LO)- activating protein (FLAP) inhibitors is a promising strategy to intervene with inflammatory, allergic and cardiovascular diseases. Virtual screening targeting FLAP based on a combined ligand-and structure-based pharmacophore model led to the identification of 1-(2- chlorobenzyl)-2-(1-(4-isobutylphenyl) ethyl)-1H-benzimidazole (7) as developable ...