- Dendritic polyglycerol as a high-loading support for parallel multistep synthesis of GABA lactam analogues
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A general route to 4-substituted azolidin-2-ones (GABA lactam analogues) on a soluble high-loading polyglycerol support has been developed and optimized. These biologically interesting compounds (anticonvulsive drugs) can be synthesized in three steps commencing from a polyglycerol supported (diethylphosphono)acetic acid and a carbonyl compound. The key features of this parallel approach are the cyclative cleavage and simple separation techniques (i.e., dialysis).
- Roller, Sebastian,Siegers, Conrad,Haag, Rainer
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p. 8711 - 8720
(2007/10/03)
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- 1-AMINOMETHYL-1,2,3,4-TETRAHYDRONAPHTHALENES
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Compounds of the formula STR1 and pharmaceutically acceptable salt thereof, wherein R 2 is selected from hydroxy and lower alkoxy, R 5 is lower alkyl, and R 11 and R 12 are independently selected from hydrogen, halo, hydroxy, methoxy, and lower alkyl, are selective . alpha.. sub.2 adrenergic receptor antagonists useful in the treatment of glaucoma.
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- 1-aminomethyl-1,2,3,4-tetrahydronaphthalenes
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The present invention provides compounds of the formula STR1 or a pharmaceutically acceptable salt thereof wherein R1 is selected from hydrogen, halo, lower alkyl, lower alkoxy, or thioalkoxy; and R2 is lower alkoxy; or R1 and R2 together form a methylenedioxy or ethylenedioxy ring; R3 and R4 are independently selected from hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, (lower alkyl)amino, (lower alkylsulfonyl)amino, and halo; and R7 is selected from the group consisting of 2- or 3-thienyl, 2- or 3-furyl, and STR2 where R13 and R14 are independently selected from the group consisting of hydrogen, hydroxy, halogen, amino, lower alkyl, lower alkoxy, lower alkylthio, methylenedioxy, or ethylenedioxy. The compounds of the present invention selectively inhibit α2 -adrenergic receptors as well as inhibit the uptake of biogenic amines and are thus useful in the treatment of certain cardiovascular and psychiatric disorders.
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- 3-thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABA(B) receptor studies
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Baclofen (β-(p-chlorophenyl)-GABA) is a selective agonist for the bicuculline-insensitive GABA(B) receptor. The search for new compounds that bind to the GABA(B) receptor is very important to clarify structural requirements. We report herein the synthesis and the binding studies of variously substituted 3-thienyl- and 3-furylaminobutyric acids. 4-Amino-3-(5-methyl-2-thienyl)butyric acid (5d) and 4-amino-3-(5-chloro-2-thienyl)butyric acid (5h) are potent and specific ligands for GABA(B) receptor. The IC50 values for the displacement of (R)-(-)-[3H]baclofen are 1.34 and 0.61 μM for 5d and 5h, respectively, as compared to 0.33 μM for baclofen.
- Berthelot,Vaccher,Flouquet,Debaert,Luyckx,Brunet
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p. 2557 - 2560
(2007/10/02)
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- Synthesis of 2-amino-4-(2-benzofuryl)Δ1 pyrrolines and study of their antidysrhythmic properties
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The synthesis of 2-amino 4(2-benzofuryl)Δ1 pyrrolines, substituted in the aromatic ring and/or on the nitrogen atom of the amino group, is described. These derivatives are obtained from 3 (2-benzofuryl) acrylic esters, on which nitromethane is added. The reduction of 4-nitrobutyric esters lead to pyrrolidinones, and then to the entitled derivatives. Some analogs, the benzofuran ring of which is replaced by another heterocycle, were also prepared. Some of them exhibit interesting antidysrhythmic properties.
- Maillard,Langlois,Vo Van,et al.
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p. 353 - 358
(2007/10/02)
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