Lipoxygenases inhibitors

Synthesis of a Class of Sulfur-Containing Lipoxygenase Inhibitors.351... 

Fluormated agents such as flurbiprofen (II), flunisal(i2), diflunisal (13), and sulindac (14), acting as prostaglandin synthesis mhibitors, have been available for some time [5] The recent introduction of flunoxaprafen (15), a lipoxygenase inhibitor, is notable It reportedly produces considerably less severe gastric disturbance [75]... 

The wide applicability of the PK reaction is apparent in the synthesis of pyrroles, for example, 45, en route to novel chiral guanidine bases, levuglandin-derived pyrrole 46, lipoxygenase inhibitor precursors such as 47, pyrrole-containing zirconium complexesand iV-aminopyrroles 48 from 1,4-dicarbonyl compounds and hydrazine derivatives. The latter study also utilized Yb(OTf)3 and acetic acid as pyrrole-forming catalysts, in addition to pyridinium p-toluenesulfonate (PPTS). 

Lipoxygenase AVNTR polymorphism in 100 bp upstream from the ATG start codon is associated with transcription efficiency. Differences in response to 5-lipoxygenase inhibitors and leucotriene receptor antagonists. 

JP04 321 624 (Hisamitsu Pharm. appl. 19.4.1991 J-prior. 19.4.1991). combination with 5-lipoxygenase inhibitors ... 

Hui, P.H., Taylor, I.K., Taylor, G.W., Rubin, P., Kesterton, J., Barnes, N.C. and Barnes, P.J. (1991). Effect of a 5-lipoxygenase inhibitor on leukotriene generation and airway responses after allergen challenge in asthmatic patients. Thorax 46, 184-189. 

Payne, A.N., Jackson, W.P., Salmon, J.A., Nicholls, A., Yeadon, M. and Garland, L.G. (1991). Hydroxamic acids and hydroxyureas as novel, selective 5-lipoxygenase inhibitors for possible use in asthma. Agents Actions 34, 189-199. 

Yeadon, M., Eve, D. and Payne, A.N. (1993c). Induction of airway hyperresponsiveness increases the potency of BW B70C, a 5-lipoxygenase inhibitor, to prevent allergic bron-choconstriction in sensitised guinea-pigs. Br. J. Pharmacol. 108, 186P. 

Lipid-lowering agents, 40 (2002) 1 5-Lipoxygenase inhibitors and their antiinflammatory activities, 29 (1992) 1 Literature of medicinal chemistry, 6 (1969) 266... 

K10. Klabunde, R. E., and Calvello, C., Inhibition of endotoxin-induced microvascular leakage by a platelet-activating factor antagonist and 5-lipoxygenase inhibitor. Shock 4, 368-372 (1995). 

Fukuishi N, Takada T, Fukuyama Y, Akagi M. Antiallergic effect of ardisiaquinone A, a potent 5-lipoxygenase inhibitor. Phytomedicine 2001 8 460-464. 

The title compound (U-66,858) and analogues are of interest as lipoxygenase inhibitors with potential application to the treatment of asthma and related disorders. 

Halicholactone (25) was reported to exhibit weak inhibitory activity against the 5-lipoxygenase from guinea pig polymorphonuclear leukocytes (IC50 = 630 pM) [38], A subsequent report detailing the three-dimensional structure of the co3 unsaturated neohalicholactone (26) described it as a potent lipoxygenase inhibitor , however, no additional experimental data were provided [39],... 

Lipoxygenase Inhibitors and their Anti-inflammatory Activities... 

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