ChemInform Abstract: 1‐(5‐Carboxyindol‐1‐yl)propan‐2‐ones as Inhibitors of Human Cytosolic Phospholipase A₂α: Synthesis and Properties of Bioisosteric Benzimidazole, Benzotriazole and Indazole Analogues.

Abstract

Enzyme inhibiting activity X 0220 1-(5-Carboxyindol-1-yl)propan-2-ones as Inhibitors of Human Cytosolic Phospholipase A 2 α: Synthesis and Properties of Bioisosteric Benzimidazole, Benzotriazole and Indazole Analogues. -The indole ring system of the cytosolic A2α(cPLA2α) inhibitor (Ia) is replaced by several nitrogen-containing analogues and the effect on the inhibitory potency, metabolic stability, and solubility is studied. The compounds with the highest metabolic stability are compounds (I). (Ib) is about seven--fold more active than the lead compound (Ia). -(BOVENS, S.; KAPTUR, M.; SCHULZE ELFRINGHOFF, A.; LEHR*, M.; Bioorg. Med.