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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

✍ Scribed by Kensuke Okuda; Hideki Muroyama; Takashi Hirota

Publisher: Journal of Heterocyclic Chemistry
Year: 2011
Tongue: English
Weight: 137 KB
Volume: 48
Category: Article
ISSN: 0022-152X
DOI: 10.1002/jhet.695

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✦ Synopsis

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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