Polycyclic N‐heterocyclic compounds,part 67: Reaction of 6,7‐substituted N‐(quinazolin‐4‐yl)amidine derivatives with hydroxylamine hydrochloride: Formation of in vitro inhibitors of pentosidine |
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| Authors: | Kensuke Okuda Hideki Muroyama Takashi Hirota |
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| Affiliation: | 1. Laboratory of Medicinal and Pharmaceutical Chemistry, Gifu Pharmaceutical University, Gifu 501‐1196, Japan;2. Laboratory of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Okayama University, Kita‐ku, Okayama 700‐8530, Japan |
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| Abstract: | Reactions of N‐(quinazolin‐4‐yl)amidines and their amide oximes with hydroxylamine hydrochloride gave cyclization products that were formed by an initial ring cleavage of the pyrimidine component followed by a ring closure formation of 1,2,4‐oxadiazole to give N‐[2‐([1,2,4]oxadiazol‐5‐yl)phenyl]formamide oximes. All isolated products were evaluated for in vitro inhibitory activity on the formation of pentosidine, which is one of representative advanced glycation end products. Some products exhibited significant inhibitory activity against pentosidine formation. J. Heterocyclic Chem., (2011). |
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