- 7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: A potential treatment for asthma
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The synthesis and pharmacological profile of a novel series of 7-methoxybenzofuran-4-carboxamides is described. Some of these compounds were found to be potent inhibitors of phosphodiesterase type 4 (PDE4). (C) 2000 Elsevier Science Ltd.
- Buckley, George,Cooper, Nicola,Dyke, Hazel J.,Galleway, Fiona,Gowers, Lewis,Gregory, Joanna C.,Hannah, Duncan R.,Haughan, Alan F.,Hellewell, Paul G.,Kendall, Hannah J.,Lowe, Christopher,Maxey, Robert,Montana, John G.,Naylor, Robert,Picken, C. Louise,Runcie, Karen A.,Sabin, Verity,Tuladhar, Bishwa R.,Warneck, Julie B. H.
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- DEVELOPING POTENT URATE TRANSPORTER INHIBITORS: COMPOUNDS DESIGNED FOR THEIR URICOSURIC ACTION
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A compound represented by the general Formula (I): a pharmaceutically acceptable salt or ester thereof, a solvate thereof, a chelate thereof, a non-covalent complex thereof, a pro-drug thereof, a deuterated radio-labeled analog thereof, and mixtures of any of the foregoing, wherein: A - K are individually selected from carbon or nitrogen; X = -O, -NR1,or -S; R1-11 are individually selected from the group consisting of-H, C1-C6 alkyl, C6-C aryl, substituted C6-C14 aryl, C1-C14-alkoxy, halogen, hydroxyl, carboxy, cyano, C1-C6-alkanoyloxy, C1-C6-alkylthio, C1-C6-alkylsulfonyl, trifluoromethyl, hydroxy, C2-C6-alkoxycarbonyl, C2-C6-alkanoylamino, -O-R12, S-R12,-SO2-Ri2, -NHSO2R12 and -NHCO2R12, wherein R12 is phenyl, naphthyl, or phenyl or naphthly substituted with one to three groups selected from C1-C6-alkyl, C6-C10 aryl,C1-C6-alkoxy and halogen, and C4-C20 hydroxyheteroaryl wherein the heteroatoms are selected from the group consisting of sulfur, nitrogen, and oxygen.
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Page/Page column 14
(2012/04/23)
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- Developing potent human uric acid transporter 1 (hURAT1) inhibitors
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The kidneys are a vital organ in the human body. They serve several purposes including homeostatic functions such as regulating extracellular fluid volume and maintaining acid-base and electrolyte balance and are essential regarding the excretion of metabolic waste. Furthermore, the kidneys play an important role in uric acid secretion/reabsorption. Abnormalities associated with kidney transporters have been associated with various diseases, such as gout. The current study utilized Xenopus oocytes expressing human uric acid transporter 1 (hURAT1; SLC22A12) as an in vitro method to investigate novel compounds and their ability to inhibit 14C-uric acid uptake via hURAT1. We have prepared and tested a series of 2-ethyl-benzofuran compounds and probed the hURAT1 in vitro inhibitor structure-activity relationship. As compared to dimethoxy analogues, monophenols formed on the C ring showed the best in vitro inhibitory potential. Compounds with submicromolar (i.e., IC 50 1000 nM) inhibitors were prepared by brominating the corresponding phenols to produce compounds with potent uricosuric activity.
- Wempe, Michael F.,Jutabha, Promsuk,Quade, Bettina,Iwen, Timothy J.,Frick, Morin M.,Ross, Ian R.,Rice, Peter J.,Anzai, Naohiko,Endou, Hitoshi
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experimental part
p. 2701 - 2713
(2011/06/25)
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- A new course of the Perkin cyclization of 2-(2-formyl-6-methoxyphenoxy)alkanoic acids. Synthesis of 2-alkyl-7-methoxy-5-nitrobenzo[b]furans
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2-Alkyl-7-methoxy-5-nitrobenzo[b]furan, 2-alkyl-9-methoxy-7-nitro-3-oxo-2,3-dihydro-5H-benzo[e][1,4]-dioxepin-5-yl acetate and 2-alkyl-5-hydroxy-9-methoxy-7-nitro-5H-benzo[e][1,4]-dioxepin-3-one were formed as a result of the cyclization of 2-(2-formyl-6-
- Kowalewska, Monika,Kwiecień, Halina
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p. 5085 - 5090
(2008/09/21)
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- Reductive, selective deoxygenation of acylbenzo[b]furans, aromatic aldehydes and ketones with NaBH3CN-TMSCl
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Aromatic aldehydes, ketones and acylbenzo[b]furans have been reductively deoxygenated with sodium cyanoborohydride and the mild electrophile chlorotrimethylsilane.
- Box, Vernon G.S.,Meleties, Panayiotis C.
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p. 7059 - 7062
(2007/10/03)
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- Intramolecular Cycloaddition Reactions of Ketene and Carbonyl Groups. A New Synthesis of Benzofurans
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(o-Carbonylphenoxy)acetyl chlorides are dehydrochlorinated to the corresponding (o-carbonylphenoxy)ketenes which undergo a cycloaddition reaction to yield tricyclic β-lactones which spontaneously decarboxylate to benzofurans.
- Brady, William T.,Giang, Frank Y.
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p. 2145 - 2147
(2007/10/02)
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