摘要/Abstract
为寻找新型杂环活性化合物，通过活性亚结构拼接方法，以硫脲和乙酰丙酮为起始原料合成4，6-二甲基嘧啶-2-硫醇，随后经醚化、肼化、环化反应，最后与取代苄氯在微波辐射中合成得到13个新型2-（取代苄硫基）-5-（4，6-二甲基嘧啶-2-硫甲基）-1，3，4-噁二唑化合物.生物活性测试结果表明，在50 μg/mL浓度下，部分化合物对尖孢炭疽病菌、枸杞炭疽病菌、草莓炭疽病菌具有较好的杀菌活性，其中取代基为3-氟时对尖孢炭疽病菌的抑制率达到80.22%；若干化合物还表现出良好的抗杜氏利什曼原虫活性，其中取代基为3-氯，4-溴，3-氟和4-叔丁基时，IC50值均低于25 μg/mL，优于对照药剂巴龙霉素.
关键词: 嘧啶环, 1,3,4-噁二唑, 硫醚, 合成, 杀菌活性, 抗杜氏利什曼原虫活性
In order to find novel biologically active heterocyclic compounds, thirteen new 2-(substitutedbenzylthio)-5-(4,6-dimethylpyrimidin-2-thiomethyl)-1,3,4-oxadiazoles were prepared with thiocarbamide and 2,4-pentanedione as the staring materials via cyclization, etherification, hydrazination, cyclization and finally a benzylation reaction under microwave irradiation condition. The preliminary bioassay results indicated that some target compounds exhibited good inhibition activity against Colletrotichum acutatum, Colletrotichum gloeosporioides and Colletrotichum fragariae at 50 μg/mL, and the inhibition rate of the compound with 3-fluoro against Colletrotichum acutatum reached 80.22%. Several compounds also showed that good antileishmanial activities against Leishmania donovani, the IC50 values of those compounds with 3-chloro, 4-bromo, 3-fluoro and 4-tert-butyl substituent respectively were all less than 25 μg/mL and were more active than the control drug paromomycin.
Key words: pyrimidine moiety, 1,3,4-oxadiazole, thioether, synthesis, antifungal activity, antileishanial activity
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