N-omega-carbethoxypentyl-4-quinolones: a new class of leukotriene biosynthesis inhibitors.
6-[(4-Quinolinyl)oxy]hexanoic acids and the corresponding esters were designed and synthesized as inhibitors of the production of arachidonic acid metabolites. The inhibitory activities were assayed in vitro by evaluation of serum leukotriene B4 and thromboxane B2 production. While all 6-[(4-quinolinyl)oxy]hexanoic acids and their esters proved to be inactive, the N-alkyl-4-quinolones, obtained as by-products in their synthesis, were found to be a new class of leukotriene biosynthesis inhibitors.
Desideri
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Dipartimento di Studi farmaceutici, Università La Sapienza di Roma, Italy.
Sestili
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I
Stein
M L
ML
Manarini
S
S
Dell'Elba
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G
Cerletti
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C
D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007975:Leukotriene B4 / Q000097:blood; D015289:Leukotrienes / Q000096:biosynthesis*; D016859:Lipoxygenase Inhibitors; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013929:Thromboxane B2 / Q000097:blood
D004791:Enzyme Inhibitors; D015289:Leukotrienes; D016859:Lipoxygenase Inhibitors; D015363:Quinolones; D007975:Leukotriene B4; D013929:Thromboxane B2