- BENZAMIDE DERIVATIVES
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Benzamides of the formula I wherein R1 and R2 each independently is hydrogen, halogen, lower alkyl, lower alkoxy, cyano, trifluoromethyl, sulfamoyl, mono(lower alkyl)sulfamoyl or di(lower alkyl)sulfamoyl or R1 and R2 on adjacent carbon atoms together are
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- Synthesis and evaluation of iodinated benzamide derivatives as selective and reversible monoamine oxidase B inhibitors
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A new series of iodinated analogues of N-(2-aminoethyl)benzamide was synthesized and evaluated for inhibitory potency and specificity toward monoamine oxidase type-B (MAO-B). Among them, N-(2-aminoethyl)-2-chloro-4-iodobenzamide hydrochloride (2d) showed high inhibitory potency and selectivity against MAO-B. The type of MAO-B inhihition by 2d was non-competitive and the inhibition constant (K(i)) was 0.80 μM. Strong and selective in vivo MAO-B inhibition by 2d was also confirmed. The brain MAO-B inhibition by 2d was reversible and the enzyme activity completely returned to the control value 24 h after administration. Compound 2d was, therefore, considered to be a candidate for advanced development as a radioiodinated ligand that may be useful for functional MAO-B studies in the living brain using single photon emission computer tomography.
- Ohmomo,Murakami,Hirata,Sugimoto,Magata,Miyahara,Tanaka,Yokoyama
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p. 1789 - 1792
(2007/10/02)
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