5-Lipoxygenase inhibitors: the synthesis and structure-activity relationships of a series of 1-phenyl-3-pyrazolidinones

…, EW Ferguson, SJ Gangell, MR Heimann…

Index: Hlasta; Casey; Ferguson; Gangell; Heimann; Jaeger; Kullnig; Gordon Journal of Medicinal Chemistry, 1991 , vol. 34, # 5 p. 1560 - 1570

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Citation Number: 33

Abstract

A series of analogues of the 5-lipoxygenase inhibitor 1-phenyl-3-pyrazolidinone (phenidone, la) has been prepared via two complementary new synthetic methods. The reaction of various electrophiles with the dianion of la or with an N-silylpyrazolidinone anion gave the desired 4-substituted pyrazolidinones (Scheme I and 11). A new procedure was developed for the resolution of 4-substituted pyrazolidinones (Scheme V). A regression ...