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A facile synthesis of 2-acyl and 2-alkylaminobenzimidazoles for 5-lipoxygenase inhibitors

Title
A facile synthesis of 2-acyl and 2-alkylaminobenzimidazoles for 5-lipoxygenase inhibitors
Authors
Lee A.H.An M.H.Choi E.H.Choo H.-Y.P.Han G.
Ewha Authors
박혜영
SCOPUS Author ID
박혜영scopus
Issue Date
2006
Journal Title
Heterocycles
ISSN
0385-5414JCR Link
Citation
Heterocycles vol. 70, pp. 571 - 580
Indexed
SCI; SCIE; SCOPUS scopus
Document Type
Article
Abstract
2-Acylaminobenzimidazoles (2a-r) have been synthesized from o-phenylenediamines (4) with benzoylcarbonimidodithioic acid dimethyl ester (5a) or isobutyrylcarbonimidodithioic acid dimethyl ester (5b) in good yield. 2-Alkylaminobenzimidazoles could be prepared by the reaction of o-Phenylenediamines (4a, b) with benzyl isothiocyanate in moderate yields 8a, b or the reaction of 2-chlorobenzimidazole (9) with benzylamines (10a, b) in moderate yield 11a, b. Finally, the carbamate derivative of 2-aminobenzimidazole (13) was prepared by the reaction with pseudourea (12) in low yield. Most of the prepared analogues were evaluated in leukotriene inhibition assay and it found that benzamide derivatives (2a-i) are quite active among others. © 2006 The Japan Institute of Heterocyclic Chemistry.
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약학대학 > 약학과 > Journal papers
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