TY - JOUR
T1 - 1,3,4-Oxadiazole-3(2H)-carboxamide derivatives as potential novel class of monoamine oxidase (MAO) inhibitors
T2 - Synthesis, evaluation, and role of urea moiety
AU - Ke, Shaoyong
AU - Li, Zhong
AU - Qian, Xuhong
PY - 2008/8/15
Y1 - 2008/8/15
N2 - A new series of 1,3,4-oxadiazole-3(2H)-carboxamide derivatives have been synthesized by direct heterocyclization reaction of substituted benzoylisocyanate with various aroylhydrazones as novel monoamine oxidase inhibitors (MAOIs). The target molecules have been identified on the basis of satisfactory analytical and spectra (IR, 1H NMR, 13C NMR, and HR-MS) data. The newly synthesized compounds were evaluated for their MAO inhibitory activity by kynuramine fluorimetric assay method. The preliminary results showed that most of the compounds have moderate inhibitory activities toward MAO at the concentration of 10-5-10-3 M. This work may provide a novel class of lead compounds with potential MAO inhibitions for further optimization.
AB - A new series of 1,3,4-oxadiazole-3(2H)-carboxamide derivatives have been synthesized by direct heterocyclization reaction of substituted benzoylisocyanate with various aroylhydrazones as novel monoamine oxidase inhibitors (MAOIs). The target molecules have been identified on the basis of satisfactory analytical and spectra (IR, 1H NMR, 13C NMR, and HR-MS) data. The newly synthesized compounds were evaluated for their MAO inhibitory activity by kynuramine fluorimetric assay method. The preliminary results showed that most of the compounds have moderate inhibitory activities toward MAO at the concentration of 10-5-10-3 M. This work may provide a novel class of lead compounds with potential MAO inhibitions for further optimization.
KW - 1,3,4-Oxadiazole-3(2H)-carboxamide
KW - Heterocycle
KW - MAO inhibitor
KW - Urea
UR - https://www.scopus.com/pages/publications/49149125590
U2 - 10.1016/j.bmc.2008.07.026
DO - 10.1016/j.bmc.2008.07.026
M3 - 文章
C2 - 18678501
AN - SCOPUS:49149125590
SN - 0968-0896
VL - 16
SP - 7565
EP - 7572
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 16
ER -