- Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors
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SAR around a known molecule with dual 5-HT1D antagonist and 5-HTtransporter inhibitory activity has led to the discovery of molecules with improved dual activity and reduced cross-reactivity toward other aminergic receptors (5-HT1B, α1, and D2).
- Bueno, Ana B.,Gilmore, Jeremy,Boot, John,Broadmore, Richard,Cooper, Jane,Findlay, Jeremy,Hayhurst, Lorna,Marcos, Alicia,Montero, Carlos,Mitchell, Stephen,Timms, Graham,Tomlinson, Rosemarie,Wallace, Louise,Walton, Leslie
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Read Online
- Squaramide-catalyzed asymmetric intramolecular oxa-michael reaction of α,β-unsaturated carbonyls containing benzyl alcohol: Construction of chiral 1-substituted phthalans
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Organocatalytic enantioselective intramolecular oxa-Michael reactions of benzyl alcohol bearing α,β-unsaturated carbonyls as Michael acceptors are presented herein. Using cinchona squaramide-based organocatalyst, enones as well as α,βunsaturated esters containing benzyl alcohol provided their corresponding 1,3-dihydroisobenzofuranyl-1-methylene ketones and 1,3-dihydroisobenzofuranyl-1-methylene esters in excellent yields with high enantioselectivities. In addition, enantioenriched 1,3-dihydroisobenzofuranyl-1-methylene ketone could be obtained from the Wittig/oxa-Michael reaction cascade of 1,3-dihydro-2-benzofuran-1-ol.
- Son, Eun Chae,Kim, Seung Yeon,Kim, Sung-Gon
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p. 6826 - 6839
(2021/05/29)
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- Dual fluorescent N-Aryl-2,3-naphthalimides: Applications in ratiometric DNA detection and white organic light-emitting devices
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A ten element matrix of 5- and 6-substituted-(2,3)-naphthalimides was prepared for the appropriate placement of substituents necessary to promote dual fluorescence (DF). As prescribed by our balanced seesaw photophysical model this matrix yielded nine new DF dyes out of a possible ten compounds. From this set of nine DF dyes, 4-fluoronaphthalic amide (37) was selected as a probe for ratiometric detection of DNA and demonstration of panchromatic emission.
- Nandhikonda, Premchendar,Heagy, Michael D.
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supporting information; experimental part
p. 4796 - 4799
(2011/01/03)
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- Pharmaceutical compounds
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This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, m and n have the values defined in claim 1, their preparation and use as pharmaceuticals.
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