- 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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- A handy and solventless direct route to primary 3-[3-aryl-1,2,4-oxadiazol- 5-yl]propionamides using microwave irradiation
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A one-step, simple and straightforward synthesis of the title amides from the corresponding carboxylic acids, urea and imidazole under microwave irradiation is described.
- Neves Filho, Ricardo A. W.,Srivastava, Rajendra M.
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p. 318 - 324
(2007/10/03)
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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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