CN114081036A - 一类医用核苷类化合物在防治农业病害中的用途 - Google Patents
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Abstract
本发明属于药物化学领域,公开了核苷类化合物在防治由油菜菌核病菌、立枯丝核病菌、番茄灰霉病菌、小麦赤霉病菌、稻瘟病菌、辣椒疫霉病菌引起的病害中的用途,其中部分化合物表现出较高的抑制作用,可用于开发杀菌先导化合物。
Description
技术领域
本发明属于药物化学领域,公开了一类核苷类化合物的新用途,具体涉及其在防治由油菜菌核病菌、立枯丝核病菌、番茄灰霉病菌、小麦赤霉病菌、稻瘟病菌、辣椒疫霉病菌引起的植物病害中的用途。
背景技术
农业面临转型升级,农业质量是绿色兴农、品牌兴农,为了守住粮食安全和生态的安全底线,对农药研发的要求也在发生着变化。目前我国常规作物病害在减轻,但是一些特殊的、新的病害却在加重,有些病害的影响程度甚至是触目惊心。因此,这种变化也为杀菌剂研发、推广和新产品应用提供了新的生长空间。希望有越来越多的新产品、新技术运用到病虫害防治中,为农业转型升级、乡村振兴作出力所能及的贡献。我国每年进口农药中数量较多的是杀菌剂,我国杀菌剂的品种和数量在我国农药产业结构中相对处于比较薄弱的环节。我国农作物病害有700多种,主要农作物病害有300多种。近3年我国农作物病害年平均发生面积17.15亿亩次。近年我国主要农作物病害发生程度总体为中等或中等偏重。
稻瘟病又进入流行周期。2016-2017年长江中下游湖南、江西等省早稻稻瘟病发生较重,东北稻区局部发生较重。稻瘟病在我国发生趋重,稻瘟病又进入一个发生流行周期。
小麦赤霉病抗药性快速发展。近年我国小麦赤霉病呈现发生范围扩大、重发频率增加、发生程度加重、危害损失增加的发生特点,且病菌抗药性呈现快速发展态势。近6年来,2010、2012、2016年偏重和大发生,偏重至大发生程度达50%,特别是长江中下游麦区,大发生频率高,危害损失大。近年来,在我国黄淮冬麦区赤霉病呈逐年加重的趋势,呈现北扩西移状态,已成为黄淮麦区常发性病害。因此,开发生物农药的活性成分会更受关注,市场前景广阔。
核苷在基因信息的复制和转录中起着关键作用,核苷类化合物具有多种生物活性,如抗肿瘤、抗菌、抗病毒等。因此,它们在化疗、抗菌和抗病毒治疗中已经被应用了几十年。核苷类似物具有一个或多个修饰性,因此可以模拟天然核苷的结构,使其足以被纳入DNA或RNA复制周期。核苷类似物被纳入DNA或RNA可能会终止链的延长或导致突变的积累。因此,进一步评价核苷类化合物的抗菌活性,为解决新农药创新难度大这一世界公认难题提供了新路径。
发明内容
本发明的目的是针对现有技术中存在的缺陷,为农业生产提供优异的杀菌剂,核苷类化合物在防治农业病害中的用途。
为实现上述目的,本发明提供了如下技术方法:一类防治由油菜菌核病菌、立枯丝核病菌、番茄灰霉病菌、小麦赤霉病菌、稻瘟病菌、辣椒疫霉病菌引起的病害的核苷类化合物,即化合物1~9,其结构式如1-9所示。
具体实施方式
为了更好地理解本发明,以下通过具体实施方式,对本发明的上述内容做进一步的详细说明。但不应将此理解为对本发明的限制。
实施例1:化合物1-9如下。
5-氟尿嘧啶核苷(1)CAS:316-46-1,纯度>98%;5'-脱氧-5-氟尿苷(2)CAS:3094-09-5,纯度>98%;尿苷(3)CAS:58-96-8,纯度>98%;阿糖尿苷(4)CAS:3083-77-0,纯度>98%;5-三氟甲基尿嘧啶(5)CAS:54-20-6,纯度>97%;5-溴-2'-脱氧尿苷(溴脲苷)(6)CAS:59-14-3,纯度>98%;2'-脱氧鸟苷(7)CAS:961-07-9,纯度>98%;更昔洛韦(8)CAS:82410-32-0,纯度>98%;5-氟-2'-脱氧脲核苷(9)CAS:50-91-9,纯度>98%。
实施例2:室内抗真菌活性测定及结果
本实验中所用的植物病原真菌为实验室保藏菌种,采用的培养基为马铃薯琼脂葡萄糖培养基(简称PDA)。
PDA培养基配方:马铃薯(去皮)200g,葡萄糖20g,琼脂15g,蒸馏水1000mL,自然pH。
PDA培养基配置方法:将马铃薯洗净去皮,称200g切成小块,蒸馏水煮20min左右,用八层纱布过滤,用蒸馏水将滤液补足至1000mL,加入15g琼脂,20g葡萄糖,搅拌使其充分溶解后,分装于三角瓶中,121℃灭菌20分钟,冷却后备用。
实验方法
1)采用菌丝生长速率法。
1、菌种活化:将植物病原菌在PDA平板上25℃培养3~6天。
2、制备药板:将PDA培养基加热熔化,冷却至45-50℃,分别加入不同浓度核苷类化合物制成带药平板。
3、接种培养:在超净台中,用打孔器在培养3~6天的菌丝边缘(生长状况尽量一致)打取菌饼(直径5mm),再用接种针接种到药板中央,然后在培养箱(25℃)中倒置培养。
4、结果测定:空白对照组菌丝长满后,采用十字交叉法测得给药组菌丝的生长直径,计算抑制率。
5、抑制率(%)=(对照菌丝直径-处理菌丝直径)/(对照菌丝直径-菌饼直径)×100
6、每个浓度设置3组平行实验。
表1核苷类化合物对植物病原真菌的抑菌活性
注:试验中每个处理设三次重复,表中数据为三次重复的平均值。
由表1测试结果可知,本发明涉及的一类核苷类化合物对油菜菌核病菌、立枯丝核病菌、番茄灰霉病菌、小麦赤霉病菌和辣椒疫霉病菌表现出较好的抑制活性。其中化合物1和化合物9对油菜菌核病菌和番茄灰霉病菌具有优异的抗菌活性。综上所述,本发明所述的核苷类化合物结构简单、对农业病菌表现出较好的抑制活性,具有进一步研究和开发价值。
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