1-(5-Carboxyindol-1-yl) propan-2-one inhibitors of human cytosolic phospholipase A2α: effect of substituents in position 3 of the indole scaffold on inhibitory potency, …

S Bovens, A Schulze Elfringhoff, M Kaptur…

Index: Drews, Andreas; Bovens, Stefanie; Roebrock, Kirsten; Sunderkoetter, Cord; Reinhardt, Dirk; Schaefers, Michael; Van Der Velde, Andrea; Schulze Elfringhoff, Alwine; Fabian, Joerg; Lehr, Matthias Journal of Medicinal Chemistry, 2010 , vol. 53, # 14 p. 5165 - 5178

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Citation Number: 18

Abstract

Indole-5-carboxylic acids with 3-aryloxy-2-oxopropyl residues in position 1 have been found to be potent inhibitors of human cytosolic phospholipase A2α (cPLA2α). In the course of structure− activity relationship studies, we investigated the effect of a substitution of indole 3 position with acyl, alkyl, and oxadiazole residues. The highest increase of inhibitory potency could be achieved by a 3-methyl-1, 2, 4-oxadiazol-5-yl-moiety. Appropriate compound 40 ...