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

被引:7
|
作者
Okuda, Kensuke [1 ]
Muroyama, Hideki [2 ]
Hirota, Takashi [2 ]
机构
[1] Gifu Pharmaceut Univ, Lab Med & Pharmaceut Chem, Gifu 5011196, Japan
[2] Okayama Univ, Fac Pharmaceut Sci, Lab Pharmaceut Chem, Kita Ku, Okayama 7008530, Japan
关键词
ADVANCED GLYCATION ENDPRODUCTS; END-PRODUCTS; 4-AMINOQUINAZOLINES; ACID;
D O I
10.1002/jhet.695
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
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.
引用
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页码:1407 / 1413
页数:7
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