- Anthranilic acid replacements in a niacin receptor agonist
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Niacin is an effective drug for raising HDL cholesterol. However, niacin must be taken in large doses and significant side effects are often observed, including facial flushing, loss of glucose tolerance, and liver toxicity. An anthranilic acid was identified as an agonist of the niacin receptor. In order to improve efficacy and provide structural diversity, replacements for the anthranilic acid were investigated and several compounds with improved properties were identified.
- Schmidt, Darby,Smenton, Abigail,Raghavan, Subharekha,Shen, Hong,Ding, Fa-Xiang,Carballo-Jane, Ester,Luell, Silvi,Ciecko, Tanya,Holt, Tom G.,Wolff, Michael,Taggart, Andrew,Wilsie, Larissa,Krsmanovic, Mihajlo,Ren, Ning,Blom, Daniel,Cheng, Kang,McCann, Peggy E.,Waters, M.Gerard,Tata, James,Colletti, Steven
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scheme or table
p. 3426 - 3430
(2010/08/07)
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- Carbanion stabilization by distal silyloxy groups. Origin of the high diastereoselectivity in the formation of quaternary centers with aryllead(IV) triacetate reagents
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(formula presented) Derivatives of methyl 5-hydroxy-2-oxo-1-cyclohexanecarboxylate react with aryllead(IV) reagents in high yield and with wide variation in diastereoselectivity. Ab initio calculations are consistent with a heretofore unrecognized attract
- Konopelski, Joseph P.,Lin, Jinzhen,Wenzel, Philip J.,Deng, Hongbo,Elliott, Gregory I.,Gerstenberger, Brian S.
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p. 4121 - 4123
(2007/10/03)
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- HIGH-PRESSURE DIELS-ALDER REACTIONS OF 2-METHYLTHIO- AND 2-ACETOXYFURAN. AN EFFICIENT ENTRY TO 4-HYDROXYCYCLOHEXANONES
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Diels-Alder reactions of 2-methylthio- and 2-acetoxyfuran were performed at 15 kbar and room temperature.The adducts were proved to be a useful precursor of 4-hydroxycyclohexanones.
- Kotsuki, Hiyoshizo,Mori, Yuichiro,Ohtsuka, Tatsuya,Nishizawa, Hitoshi,Ochi, Masamitsu,Matsuoka, Kiyoshi
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p. 2347 - 2350
(2007/10/02)
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