LTB Antagonists Related to HAPType LTD4 Antagonists

A team at Eli Lilly discovered that moving the alkyl chain from the hydroxyacetophenone (HAP) 3-position, as found in FPL-55712 (28), resulted in selective LTB, antagonists. For example, LY255283 (41) inhibited LTB4 binding

to neutrophils with an IC„ value of 87 nM

(264). Further work in this class yielded LY293111 (42), which was active in blocking LTB4-induced bronchoconstriction in vivo

(265). A publication on LY293111 has appeared describing its pharmacology in vivo

(266). Unfortunately, the compound was not effective in clinical trials in asthmatics.

The Searle group apparently started with FPL-5512 analogs and arrived at SC 53228 (43), which antagonized LTB4 binding with an

IC50 value of 1.3 nM. The compound was also active in blocking PMA-induced ear edema (<2.5 mg/kg).

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