LT synthesis inhibitors

Leukotriene (LK) Leukotriene is the primary bronchoconstrictor. This increases migration of eosinophil, increases mucous production and increases edema in the bronchi, resulting in bronchoconstriction. There are two types of leukotriene modifiers LT receptor antagonists and LT synthesis inhibitors. Both reduce inflammatory symptoms of asthma. Leukotriene modifiers include ... 

The identification of FLAP as the molecular target for MK-886 led to the establishment of radioligand binding assays to identify inhibitors that were more potent than MK-886 and were derived from novel chemical series [68]. These studies resulted in the identification at Merck Frosst of quinoline-based FLAP antagonists such as L-674,573 and quinoline-indole hybrids (termed quindoles) such as MK-591 [45,46,69,70]. A number of companies have now identified LT synthesis inhibitors that are known to interact with FLAP, such as Bay X 1005, WAY 50,295 and REV-5901 [14,43,47,48,71,72]. 

The effects of leukotrienes can be blocked at several levels. Inhibitors of FLAP or 5-LO inhibit LT synthesis at all levels. However, FLAP antagonists developed to date have been too hepatotoxic for human use. Zileuton, a 5-LO synthase inhibiting drug, also demonstrated some hepatotoxicity in a small percentage of patients, which was nonetheless entirely reversible. However, the short half-life of this compound requires four times daily... 

JG Taylor, TP Owen Jr, LT Koonce, and CH Haigler. Dispersed Lignin in Tracheary Elements Treated with CeUnlose Synthesis Inhibitors Provides Evidence that Molecules of the Secondary Cell Wall Mediate Wall Patterning. The Plant Journal 2 959-970, 1992. 

The total synthesis of kasugamydn, a two-unit type aminoglycoside, produced by Streptomyces kasugalusis, has also been described.lt is a potent inhibitor of Peri-cularia oryzae, a plant pathogen... 

Rifampicin is also an inhibitor of the synthesis of a number of phages and viruses. It has been demonstrated that the RNA polymerase, which transcribes phage p 22 following infection of Bacillus subtilis, retains the rifampicin sensitivity of the host cell enzyme , Rifampicin also inhibits the formation of infectious vaccinia virus and viral particles. Whereas virion formation is completely inhibited neither the synthesis of RNA and protein nor the activity of in vitro RNA polymerase associated to the virion is affected lt>, Rifampicin inhibits the multiplication of poxvirus in vitro and in vivo. The side chain of this antibiotic derivative appears to be essential for the anti-viral effect and anti-trachomal activity found in... 

Robina et al. reported synthesis and biological study of 5-galactosides containing a polyhydrojgrallq lfuran as a potential inhibitors of cholera toxin (CT) and heat-labile toxin (LT). The interaction of the best candidates with CT and LT was studied by weak affinity chromatography (WAC) and saturation transfer differenee NMR experiments. 

Uses Intermediate for cationic surfactants, softeners, emulsifiers, dispersants, organic synthesis corrosion inhibitor for metals Properties Lt. yel. solid iodine no. 50 min. amine no. 110-120 100% cone. Nissan Amine AB [NOF]... 

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