102234-44-6Relevant articles and documents
7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: A potential treatment for asthma
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.
, p. 2137 - 2140 (2000)
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.
Developing potent human uric acid transporter 1 (hURAT1) inhibitors
Wempe, Michael F.,Jutabha, Promsuk,Quade, Bettina,Iwen, Timothy J.,Frick, Morin M.,Ross, Ian R.,Rice, Peter J.,Anzai, Naohiko,Endou, Hitoshi
experimental part, p. 2701 - 2713 (2011/06/25)
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.
Reductive, selective deoxygenation of acylbenzo[b]furans, aromatic aldehydes and ketones with NaBH3CN-TMSCl
Box, Vernon G.S.,Meleties, Panayiotis C.
, p. 7059 - 7062 (2007/10/03)
Aromatic aldehydes, ketones and acylbenzo[b]furans have been reductively deoxygenated with sodium cyanoborohydride and the mild electrophile chlorotrimethylsilane.
