- 9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides as potent, orally available mGlu1 receptor enhancers
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Small molecule mGluR1 enhancers based on the lead compound (9H-xanthene-9-carbonyl)-carbamic acid butyl ester derived from random-screening hit diphenylacetyl-carbamic acid ethyl ester were designed and synthesized as useful pharmacological tools for the study of the physiological roles mediated by mGlu1 receptors. The synthesis and the structure-activity relationship of this new class of positive allosteric modulators of mGlu1 receptors will be discussed in detail.
- Vieira, Eric,Huwyler, Joerg,Jolidon, Synese,Knoflach, Frederic,Mutel, Vincent,Wichmann, Juergen
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p. 4628 - 4631
(2007/10/03)
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- A generalized synthesis of 3-amino-5-aryl-, 3-amino-5-polyfluorophenyl-, and 3-amino-5-alkyl-1,2,4-oxadiazoles through ring-degenerate rearrangements
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A generalized synthesis of 3-amino-5-aryl-, 3-amino-5-polyfluorophenyl- and 3-amino-5-alkyl-1,2,4-oxadiazoles has been developed starting from the 3-amino-5-methyl-1,2,4-oxadiazole as a common synthon. Aroylation or alkanoylation of this aminooxadiazole,
- Buscemi, Silvestre,Pace, Andrea,Frenna, Vincenzo,Vivona, Nicolo?
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p. 811 - 823
(2007/10/03)
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- A generalized and efficient synthesis of 3-amino-, 3-(N-alkylamino)-, 3-(N,N-dialkylamino)-5-alkyl-1,2,4-oxadiazoles by irradiation of 3-alkanoylamino-4-phenyl-1,2,5-oxadiazoles (Furazans)
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Irradiation of 3-alkanoylamino-4-phenyl-1,2,5-oxadiazoles (furazans) at λ = 310 nm in methanol and in the presence of ammonia, primary or secondary aliphatic amines produced excellent yields of 3-amino-, 3-(N-alkylamino)-, 3-(N,N-dialkylamino)-5-alkyl-1,2
- Buscemi,Vivona,Caronna
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p. 917 - 919
(2007/10/02)
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