European journal of medicinal chemistry

Structure-activity relationship studies on (4-acylpyrrol-2-yl) alkanoic acids as inhibitors of the cytosolic phospholipase A 2: variation of the alkanoic acid substituent, the …

M Lehr

Index: Lehr European Journal of Medicinal Chemistry, 1997 , vol. 32, # 10 p. 805 - 814

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Citation Number: 13

Abstract

(4-Acylpyrrol-2-yl) alkanoic acid derivatives were prepared and evaluated for their ability to inhibit the cytosolic phospholipase A2 of intact bovine platelets. To define the structural requirements for enzyme inhibition, the alkanoic acid group, the acyl residue and the position of the pyrrole nitrogen relative to the pyrrole substituents were varied systematically. Inhibition of cPLA2 was best by compounds containing a free acetic acid or propionic acid ...