- Development of fluorinated CB2 receptor agonists for PET studies
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A convergent strategy was followed to modify systematically carbazole based CB2 receptor ligands. The length of the N-(fluoroalkyl) group (n in 7), the length of the alkanamide (m in 7) and the substitution pattern of the phenyl moiety (X and Y in 7) were varied systematically. The highest CB 2 affinity was found for the 2-fluoroethyl substituted carbazole derivative 20a (Ki = 5.8 nM) containing the propionamide and the 2-bromo-4-fluorophenyl moiety. According to docking studies 20a fits nicely into the binding pocket of the CB2 receptor, but elongation of the fluoroethyl side chain leads to a different binding mode of the ligands. The high CB2 affinity together with the high selectivity over the CB 2 subtype qualifies the fluoroethyl derivative 20a to be developed as a PET tracer.
- Lueg, Corinna,Schepmann, Dirk,Günther, Robert,Brust, Peter,Wünsch, Bernhard
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p. 7481 - 7498
(2013/11/19)
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- Improved microwave-mediated synthesis of 3-(3-aryl-1,2,4-oxadiazol-5-yl) propionic acids and their larvicidal and fungal growth inhibitory properties
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The synthesis of 3-(3-aryl-1,2,4-oxadiazol-5-yl)propionic acids from arylamidoximes and succinic anhydride under focused microwave irradiation conditions is described. The new synthetic method furnished the desired products in 2-3 min and good yields. Fur
- Neves Filho, Ricardo Antonio Wanderley,Da Silva, Cecilia Aguiar,Da Silva, Clecia Sipriano Borges,Brustein, Vanessa Passos,Navarro, Daniela Maria Do Amaral Ferraz,Dos Santos, Fabio Andre Brayner,Alves, Luiz Carlos,Cavalcanti, Marilia Gabriela Dos Santos,Srivastava, Rajendra Mohan,Carneiro-Da-Cunha, Maria Das Gracas
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experimental part
p. 819 - 825
(2010/01/19)
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- Synthesis and structure determination of N,N-diethyl-3-[3-aryl-1,2,4- oxadiazol-5-yl]propionamides
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An efficient and facile synthesis of six new 1,2,4-oxadiazoles (6a-f) with a tertiary amide group attached on the side-chain, in high yield, is described. Correct assignments of side-chain methylene, methyl protons, and carbon signals have been made with the assistance of COSY, NOESY and HETCOR NMR experiments.
- Srivastava, Rajendra Mohan,Da Concei??o Pereira, Maria,Hallwass, Fernando,Pacheco, Carlos R. N.
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p. 2961 - 2967
(2007/10/03)
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