- Tricyclic heterocycles display diverse sensitivity to the A147T TSPO polymorphism
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The 18 kDa translocator protein (TSPO) is a target for the development of imaging agents to detect neuroinflammation. The clinical utility of second-generation TSPO ligands has been hindered by the presence of a polymorphism, rs6971, which causes a non-co
- Sokias, Renee,Werry, Eryn L.,Alison Cheng, Hei Wun,Lloyd, James H.,Sohler, Greta,Danon, Jonathan J.,Montgomery, Andrew P.,Du, Jonathan J.,Gao, Quanqing,Hibbs, David E.,Ittner, Lars M.,Reekie, Tristan A.,Kassiou, Michael
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- BENZIMIDAZOLONE CHYMASE INHIBITORS
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Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase.
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Page/Page column 224-225
(2009/01/20)
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- Dibenzo-fused seven-membered nitrogen heterocycles by a tandem reduction-lactamization reaction
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Efficient syntheses of dibenz[b,f][1,4]oxazepin-11(10H)-one, 5,10-dihydro-11H-dibenzo[b,e][1,4]-diazepin-11-one and 5,11-dihydro-6H-dibenz[b, e]azepin-6-one are described using a tandem reduction-lactamization sequence. Precursors for these ring systems are available in 1-3 steps using nucleophilic aromatic substitution and Ullmann coupling methodology. Direct reduction-lactamization of these compounds using iron powder in acetic acid at 115° affords the target heterocycles in ≥90% yield.
- Bunce, Richard A.,Schammerhorn, James E.
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p. 1031 - 1035
(2007/10/03)
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- COENZYME MODELS. PART 45. SYNTHESIS OF ATROPISOMERIC FLAVINS AND THEIR NOVEL REDOX-INDUCED RACEMISATION
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Seven (5-carba)isoalloxazines with restricted rotation about the C(1')-N(10) single bond were synthesized for the first time.They were optically resolved by a liquid chromatographic method.Six of these atropisomers (92.1-100 percent enantiomeric excess) (
- Shinkai, Seiji,Nakao, Hideki,Kuwahara, Itsuko,Miyamoto, Megumi,Yamaguchi, Toshiro,Manabe, Osamu
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p. 313 - 320
(2007/10/02)
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- Metal Template Reactions. XVII. The Attempted Dimerization of Amino Carbonyl Compounds Containing a Supporting Donor Atom
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Attempts to effect metal template condensative dimerizations of the amino aldehydes (4), (11) and (12) and the amino ketone (24) have been unsuccessful.Oxidation of the alcohol (9) did not allow isolation of the aldehyde (4).The alcohol (17) underwent oxi
- Black, David St. C.,Rothnie, Neil E.
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p. 1149 - 1157
(2007/10/02)
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