Folate antagonists.<b>16</b>. Antimalarial and antibacterial effects of 2,4-diamino-6-[(heterocyclic)thio, sulfinyl, and sulfonyl]quinazolines
作者:Edward F. Elslager、Patricia Jacob、Judith Johnson、Leslie M. Werbel
DOI:10.1002/jhet.5570170127
日期:1980.1
mercaptoheterocycles provided the corresponding 2-nitro-5-[(heterocyclic)thio]benzonitriles. Reduction to the amine followed by cyclization with chloroformamidine hydrochloride afforded a series of 2,4-diamino-6-[(hetero-cyclic)thio]quinazolines. Bromination, oxidation, and amidine formation were accomplished with 2,4-diamino-6-[(4-phenyl-2-thiazolyl)thio]quinazoline (23) to provide additional analogs. Several of
5-氯-2-硝基苄腈与各种巯基杂环的反应提供了相应的2-硝基-5-[(杂环)硫代]苄腈。还原成胺,然后用氯甲am盐酸盐环化,得到一系列2,4-二氨基-6-[(杂环)硫代]喹唑啉。用2,4-二氨基-6-[(4-苯基-2-噻唑基)硫代]喹唑啉(23)完成溴化,氧化和am的形成,以提供另外的类似物。这些化合物中的几种对小鼠的伯氏疟原虫的药物敏感性品系表现出抑制性的抗疟疾活性。