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

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Title
A facile synthesis of 2-acyl and 2-alkylaminobenzimidazoles for 5-lipoxygenase inhibitors
Author(s)
Jin Ha Lee; Mi Hyun Ahn; E H Choi; H Y Park Choo; G Han
Bibliographic Citation
Heterocycles, vol. 70, no. 1, pp. 571-580
Publication Year
2006
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.
ISSN
0385-5414
Publisher
Elsevier
DOI
http://dx.doi.org/10.1002/chin.200723117
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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