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作者合成了有4-取代-1-氨基硫脲、3,4-二取代噻唑啉和3-取代-4-噻唑烷酮侧链的三类可能具有抗革兰氏阳性菌及抑制真菌活性的4-氧代喹唑啉衍生物。以4-(2-甲基-4-氧代喹唑啉-3-基)苯甲酰肼(1)为中间体,与有取代烷基、芳基或芳烷基的异硫氰酸酯在乙醇中回流反应得到所需的氨基硫脲2,收率70～85％。2与溴乙酰苯或溴乙酸乙酯反应,得到噻唑啉3(收率51～64％)或噻唑烷酮4(收率87～92％)。它们大部分在体外均具有明显的抗革兰氏阳性细
The authors synthesized three classes of compounds that may have Gram-positive bacteria and inhibit fungal activity with 4-substituted-1-thiosemicarbazides, 3,4-disubstituted thiazolines and 3-substituted-4-thiazolidinone side chains 4-oxoquinazoline derivatives. An isothiocyanate having a substituted alkyl, aryl or aralkyl group as an intermediate with 4- (2-methyl-4-oxoquinazolin-3-yl) benzohydrazide The reaction was refluxed in ethanol to give the desired thiosemicarbazide 2 in 70-85% yield. 2 with bromoacetophenone or ethyl bromoacetate to give thiazoline 3 (51-64% yield) or thiazolidone 4 (yield 87-92%). Most of them have significant anti-Gram-positive fits in vitro