| Reference | [1]. Stock, N., Baccei, C., Bain, G., Broadhead, A., Chapman, C., Darlington, J., King, C., Lee, C., Li, Y., Lorrain, D.S. and Prodanovich, P., 2010.<br />
5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2, 3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2, 2-dimethyl-propionic acid (AM679)—A potent FLAP inhibitor.<br />
Abstract: AM643 (compound 6, 3-{3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid) was identified as a potential candidate for formulation as a topical agent for the treatment of skin disorders involving leukotriene production. Dermal application of 6 using a prototypical vehicle in a murine ear arachidonic acid model showed significant reduction in the concentrations of leukotrienes in mouse skin with concomitant reduction in ear swelling.<br />
Bioorganic & medicinal chemistry letters, 20(1), pp.213-217.<br />
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[2]. El-Ahl, A.A., Ismail, M.A. and Amer, F.A., 2003.<br />
Synthesis and Transformations of 2-Substituted Tetrahydro-4 H-benzo [4, 5] thieno [2, 3-d][1, 3] oxazines and 2, 3-Disubstituted Hexahydrobenzo [4, 5] thieno [2, 3-d] pyrimidines.<br />
Abstract: 3-(4-Oxo-5,6,7,8-tetrahydro-4 H -benzo[4,5]thieno[2,3-d][1,3]oxazin-2-yl)propanoic acid and its ethyl ester 6a , b have been prepared via succinoylation of ethyl 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate 1 , followed by ester hydrolysis, selective esterification, and acetic anhydride induced cyclization of the thiophenecarboxylic acid derivatives 3 , 5 . Reaction of 1 with diethyl malonate gave the malonic acid diamide 7 , which on ester hydrolysis followed by acetic anhydride induced water elimination furnished the 2-substituted 4 H -benzo[4,5]thieno[2,3-d][1,3]oxazine derivative 10 in high yield. A series of new benzo[4,5]thieno[2,3-d]pyrimidines 11-19 , which bear a propanoic acid substituent in the 2-position and an amino, aryl, aminosugar, and arylmethylideneamino-substituents in the 3-position have been prepared via the reaction of 6a , b with hydrazine hydrate or aromatic amines followed by treatment with aromatic aldehydes, isatin, or aldoses. The aldimines 18a-d underwent unprecedented acid catalyzed tandem cyclization-transannular aldehyde extrusion into octahydro-1 H -benzo[4',5']thieno[2',3':4,5]pyrimido[1,2-b]pyridazines 21 . Two other unequivocal approaches for 21 also have been explored, either by treatment of the amino acid derivative 11 with thionyl chloride or by thermal cyclization of the amino ester derivative 12 .<br />
Phosphorus, Sulfur, and Silicon and the Related Elements, 178(2), pp.245-259.<br />
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[3]. Panico, A., Cardile, V., Santagati, A. and Gentile, B., 2001.<br />
Thienopyrimidine derivatives prevent cartilage destruction in articular disease.<br />
Abstract: The effects of a series of thienopyrimidine derivatives on the prevention of cartilage destruction in articular disease were investigated. Anti-degenerative activity was assayed on culture of nasal pig cartilage in the presence or in the absence of interleukin 1β (IL-1β). The amount of glycosaminoglycans (GAGs) and the production of nitric oxide (NO) in the culture medium were determined. Some thienopyrimidine derivatives, in the presence of IL-β, blocked the cartilage breakdown by inhibiting both the NO production and GAGs release in a dose-dependent manner.<br />
Il farmaco, 56(12), pp.959-964.
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