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2-氨基-4-(肼基和羟氨基)-6-[(芳基)硫代]喹唑啉的合成及其抗疟和抗肿瘤作用

Synthesis and antimalarial and antitumor effects of 2-amino-4-(hydrazino and hydroxyamino)-6-[(aryl)thio]quinazolines.

作者信息

Werbel L M, Degnan M J

机构信息

Warner-Lambert/Parke-Davis Pharmaceutical Research, Ann Arbor, Michigan 48105.

出版信息

J Med Chem. 1987 Nov;30(11):2151-4. doi: 10.1021/jm00394a038.

DOI:10.1021/jm00394a038
PMID:3669022
Abstract

A variety of analogues of 2,4-diamino-6-[(aryl)thio]quinazolines with known antimalarial properties were prepared wherein the 4-amino group was replaced by hydrazino and hydroxyamino moieties. Such changes were found to reduce markedly the antimalarial and antitumor properties of this series.

摘要

制备了多种具有已知抗疟特性的2,4-二氨基-6-[(芳基)硫代]喹唑啉类似物,其中4-氨基被肼基和羟氨基部分取代。发现这种变化显著降低了该系列的抗疟和抗肿瘤特性。

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Synthesis and antimalarial and antitumor effects of 2-amino-4-(hydrazino and hydroxyamino)-6-[(aryl)thio]quinazolines.2-氨基-4-(肼基和羟氨基)-6-[(芳基)硫代]喹唑啉的合成及其抗疟和抗肿瘤作用
J Med Chem. 1987 Nov;30(11):2151-4. doi: 10.1021/jm00394a038.
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[Studies on antimalarial agents. XVI. Syntheses and antimalarial activities of 2, 4-diamino-6-[(substituted phenyl)thio, sulfinyl and sulfonyl] quinazolines].[抗疟药研究。十六。2,4-二氨基-6-[(取代苯基)硫基、亚磺酰基和磺酰基]喹唑啉的合成与抗疟活性]
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[Synthesis and antimalarial as well as antitumor activities of 2,4-diamino-6-(N-methyl-substituted benzylamino) quinazolines].2,4-二氨基-6-(N-甲基取代苄基氨基)喹唑啉的合成、抗疟及抗肿瘤活性
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Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.叶酸拮抗剂。13. 2,4 - 二氨基 - 6 - [(α,α,α - 三氟 - 间甲苯基)硫代]喹唑啉及相关的2,4 - 二氨基 - 6 - [(苯基和萘基)硫代]喹唑啉,一类具有非凡抗疟和抗菌作用的独特抗代谢物。
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Synthesis of 5-substituted quinazolines as potential antimalarial agents.作为潜在抗疟药物的5-取代喹唑啉的合成。
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