- Phenyl acetate derivatives, fluorine-substituted on the phenyl group, as rapid recovery hypnotic agents with reflex depression
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We report the synthesis of novel, potentially hypnotic fluorine-substituted phenyl acetate derivatives. We describe the structure-activity relationship that led us to the promising derivative: ethyl 2-(4-(2-(diethylamino)-2-oxoethoxy)-5-ethoxy-2-fluorophenyl) acetate (55). The unique pharmacological features of compound 55 are its relatively high affinity for the GABAA receptor, together with a unique affinity for the NMDA receptor, different to propanidid and AZD3043. In animal models, compound 55 showed stronger hypnotic potency and longer duration of LORR than propanidid and AZD3043, but also maintained a rapid recovery time to walking and behavioral recovery. In particular, compound 55 displayed reflex depression during infusion.
- Zhang, Heng,Xu, Xiangqing,Chen, Yin,Qiu, Yinli,Liu, Xin,Liu, Bi-Feng,Zhang, Guisen
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p. 524 - 539
(2014/12/11)
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- QSAR study for?a?novel series of?ortho disubstituted phenoxy analogues of?α1-adrenoceptor antagonist WB4101
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On the basis of the affinities at the α1a-, α1b- and α1d-adrenoceptors and the 5-HT1A receptor of a previous series of sixteen 2-[(2-phenoxyethyl)aminomethyl]-1,4-benzodioxanes ortho monosubstituted at the pheno
- Pallavicini,Fumagalli,Gobbi,Bolchi,Colleoni,Moroni,Pedretti,Rusconi,Vistoli,Valoti
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p. 1025 - 1040
(2007/10/03)
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- Facile and regioselective dealkylation of alkyl aryl ethers using niobium(V) pentachloride
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A simple and facile method for the cleavage of carbon-oxygen bonds promoted by niobium pentachloride(V) is described. Excellent yields and regioselectivities were observed with various alkyl aryl ethers to give the phenols. NMR studies revealed the formation of monoaryloxy niobium salt(V), and a neighboring-group effect may play a significant role in the regioselectivity. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.
- Sudo, Yukinori,Arai, Shigeru,Nishida, Atsushi
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p. 752 - 758
(2007/10/03)
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- SYNTHESIS OF FLUORINATED BIPHENYLS VIA ARYNE REACTION
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Synthesis of fluorinated biphenyls via attack of a benzyne by an anion of 3-fluoroanisole.
- Adejare, Adeboye,Miller, Duane D.
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p. 5597 - 5598
(2007/10/02)
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- 6-PHENYL THIO- AND 6-CYCLOHEXYL THIO-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINES
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Mercapto substituted-2,3,4,5-tetrahydro-1H-3-benzazepines having dopamine receptor blocking activity are prepared from o-quinones or via standard preparative procedures.
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