SYP-Z048 啶菌噁唑

SYP-Z048 is a new fungicide developed by the Shenyang Research Institute of Chemical Industry. The oralLD50 of SYP-Z048 was 926 and 1260 mg/kg in male and female mice, respectively. Simultaneous studies wereconducted on bone marrow micronucleus and spermatocyte chromosome aberration in mice, yielding negative resultsand no evidence of mutagenic effects.

A synergistic combination of thiram and SYP-Z048 (5:1) has been selected using the mycelial growth rate tests on the Botrytis cinerea strains from different regions of Baoding and Chengde.The effects of the combination of thiram and SYP-Z048 on the spore germination rate,the inhibitory activity of sclerotia,and the contents of the mycelium content has also been studied.The 5:1 combination showed significant inhibitory effects on the spore germination,emergence and germination of sclerotia and soluble sugar,soluble protein content is significant,in contrast with the control and the compound used alone.The inhibitory effects of 5:1 combination on lesion diameters,infection rates and spore germination rates was significantly better than that in control and single compound used alone.To sum up,the combination of thiram and SYP-Z048 has a synergistic inhibitory activity on Botrytis cinerea.

The Study on Sensitivity and Resistant Risk Assessment of Botrytis Cinerea to SYP-Z048

Gray Mould, one of major fungal diseases on vegetable and fruit crops, can cause severe losses of vegetables. The control of gray mould relies on application of chemical synthesized fungicides. But the contradict between chemical control and occurrence of the fungal resistance to the fungicides is standing out increasingly. SYP-Z048, a novel fungicide, which was developed by Chemical Institute of Shenyang , has special mode of action to Botrytis cinerea. It has never been used in Hebei province. In the view of widespreading occurrence of resistance to the most of systemic fungicides in Botrytis cinerea , the study of resistance of Botrytis cinerea to novel fungicide is in critical request .The results were shown as follows about cross-resistance between other fungicides and SYP-Z048 ,baseline-sensitivity to SYP-Z048, risk resistance assessment to SYP-Z048 in the lab,the physiological and biochemical parameters comparison of resistant mutants and parental isolates to SYP-Z048,and the synergistic interaction of mixing combinations between SYP-Z048 and pyrimethanil.1. Sensitivity to pyrimethanil, procymidone, carbendazim, and difenoconazole was determined of 11 SYP-Z048-sensitive strains and 3 SYP-Z048-resistant strains. Correlation coefficient is 0.0069,0.0006,0.0007 and 0.0018 respectively in linear regression analysis between EC50 values of SYP-Z048 and pyrimethanil, procymidone, carbendazim, and difenoconazole, which indicated that the correlation between EC50 values of SYP-Z048 and the other four fungicides is poor; there was no positively coorelaled cross-resistance between SYP-Z048 and the four fungicides.2.The baseline-sensitivity of Botrytis cinerea to SYP-Z048 was established. The sensitivity to SYP-Z048 of a total of 102 single-spore isolates, accquired by single-spore from the leaves and fruits of tomato and cucumber infected by Botrytis cinerea collected from greenhouse and plastic tunnels in Baoding, Langfang, Chengde and Hengshui of Hebei Province where SYP-Z048 was never used, was determined by mycelial growth rate inhibition test. The frequnency of EC50 values distributed as a unimodal curve, ranging from 0.0460 to 0.1991μg/mL, with a mean value of (0.1182±0.0363)μg/mL. No subpopulation resistant to SYP-Z048 appeared among these isolates, so the data could be used as baseline sensitivity of Botrytis cinerea to SYP-Z048.3. Seven SYP-Z048-resistant mutants were obtained through ultraviolet irradiation. It was found that the resistant mutants significantly decreased in the colonies diameter, mycelial weight,sporulation, sclerotial number and pathogenicity, compared with their parental single-spore isolates. And the resistance level of SYP-Z048-resistant mutants receded as the resitant mutants to SYP-Z048 was subcultured on PDA plate in absence of fungicides. Thus, a low or moderate risk of resistance to SYP-Z048- is supposed to exist in Botrytis cinerea in fields.4. Through test of conductivity of amended with plugs of SYP-Z048-resistant mutants and their parental isolates for the same time, it was found that osmosis of resistant mutants were higher than their parental isolates. Besides, SYP-Z048-resistant mutants were extremely sensitive to high concentration of glucose and NaCl agar. The resistant mechanism of Botrytis cinerea to SYP-Z048 will be refered to this results.5. The highest synergistic ratio of mixtures was found to be 1:9 in the 52 mixtures of SYP-Z048 with pyrimethanil through test of the synergistic interaction of the mixtures of SYP-Z048 with pyrimethanil against mycelial growth of Botrytis cinerea.

啶菌恶唑

英文名:(SYP-Z048) 　
中文商品名称: 灰霉净
英文化学名称: 5--2,3-dimethyl-3-(pyridine-3)-oxazoline
中文化学名称: N-甲基-3-(4-氯)苯基-5-甲基-5-吡啶-3-甲基-噁唑啉　+
分子式: C16H17ClN2O
剂型:25％乳油。
性状描述: 原药外观为稳定的均相液体，无可见的悬浮物和沉淀物。易溶于丙酮、氯仿、乙酸乙酯、乙醚，微溶于石油醚，不溶于水。在水中、日光或避光下稳定。
毒 理 学 性 质: /LC50 急性经口LD50：大鼠>4640mg/kg；急性经皮LD50：大鼠>2150mg/kg\\
啶菌噁唑是沈阳化工研究院创制的具有自主知识产权的农用杀菌剂,主要用于植物灰霉病的防治。 本试验分别以大鼠、小鼠、兔、豚鼠为对象研究了啶菌嗯唑原药的毒性,具有重要的经济意义和生态意义。结果如下： 1.啶菌噁唑急性毒性研究 本试验以SD大鼠为对象研究啶菌噁唑原药的急性经口和经皮毒性,测定了啶菌噁唑原药对大鼠经口和经皮的半数致死剂量。结果表明：啶菌噁唑原药对8周龄雄性大鼠经口LD50为2000mg／kg体重,经皮LD502000 mg／kg体重。以大耳白兔为对象研究啶菌噁唑原药的急性眼刺激和皮肤刺激毒性,结果表明：大耳白兔急性眼刺激强度为无刺激性,急性皮肤刺激强度为无刺激性。另以豚鼠为试验动物进行皮肤致敏试验,采用Buehler赶贴法检测啶菌噁唑原药对豚鼠皮肤致敏率,结果表明啶菌噁唑原药对豚鼠皮肤为弱致敏物。 2.啶菌噁唑致畸毒性研究 以SD大鼠为对象研究啶菌嗯唑原药的胚胎毒性和致畸作用。试验设20、100、500mg／kg三个剂量组、阴性对照组和2mg／kg敌枯双阳性对照组,给药时间为大鼠妊娠后第6天至第15天。试验结果表明：以500mg／kg剂量经口投予SD妊娠大鼠,受孕大鼠的体重增长缓慢,但对胎鼠无影响。试验结果为啶菌噁唑对胎鼠无胚胎毒性与致畸作用。 3.啶菌噁唑亚慢性毒性研究 以啶菌恶唑原药对S.D大鼠进行了13周喂饲毒性试验,试验设计1个对照组及3个剂量组,分别为0、40、200、1000mg／kg饲料,每组雌雄动物均为10只。13周连续喂饲期间对动物进行体重、摄食测定及临床症状观察；喂饲期结束进行动物血液常规、血液生化、尿液常规、脏器重及病理学检测,并对各项指标进行统计学处理。计算样品摄入量。测出最大无作用剂量雄性为17.53±2.15mg／kg／day,雌性为16.57±1.03mg／kg／day。 4.啶菌噁唑慢性致癌毒性研究 以啶菌噁唑原药对SD大鼠进行了2年喂饲慢性毒性与致癌联合试验,试验设计1个对照组及3个剂量组,分别为0、40、200、600mg／kg饲料,每组雌雄动物均为80只。2年连续喂饲期间对动物进行体重、摄食测定及临床症状观察；并于26、52、78、104周(结束)进行动物的尿液常规、血液常规、血液生化、脏器重及病理学检测。并对各项指标进行统计学处理。计算样品摄入量。试验结果如下：啶菌嗯唑原药对SD大鼠2年喂饲给药最大无作用剂量雄性为200mg／kg饲料,雌性为200mg／kg饲料；计算化学品摄入量结果雄性为10.0±0.9mg／kg／day,雌性为13.3±1.7mg／kg／day；未发现致癌性改变。
作用特点: 属甾醇合成抑制性杀菌剂，通过根部施药能有效地控制地上叶不病害的发生与危害。具有广谱的杀菌活性，同时具有保护和治疗作用以及良好的内吸性。
应用:　在离体情况下，对植物病原菌有极强的杀菌活性。通过叶片接种防治黄瓜灰霉病，在125～500mg（a.l.）／L的浓度下防治效果在90.67％～1O0％之间。本品乳油对小麦、黄瓜白粉病也有很好的防治作用，在125～500mg（a.i.）／L的浓度下对黄瓜白粉病的防治效果在95％以上，对白粉病的杀菌活性与腈菌唑基本相似，高于三唑酮。本品对由灰葡萄孢菌引起的灰霉病也有很好的防治效果，杀菌活性高于目前生产上推广和使用的其他化学药剂。　田间试验结果表明在200～40Og（a.i.）／hm2的剂量下对众多类型的灰霉病均具有很好的防效。