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A new antibiotic designated compound number 616

机译:新的抗生素称为化合物编号616

摘要

PICT:0832391/IV (b)/1 A new antibiotic designated "compound number 616" is produced by cultivating a compound 616-producing strain of streptomyces parvisporogenes, e.g. S. parvisporogenes ATCC 12568 in an aqueous nutrient medium containing a source of carbon and a source of organic nitrogen under submerged aerobic conditions. Specified sources of (a) carbon are sugars such as dextrose, starch and glycerol, (b) nitrogen, are casein, casein hydrolyzate, corn meal, peanut meal, soybean meal, cottonseed meal, wheat gluten, lactalbumin and tryptone. Other components are (a) growth substances, e.g. yeast extract, distillers' solubles and molasses butanol fermentation residues; (b) mineral salts, e.g. sodium chloride, potassium phosphate, sodium nitrate and magnesium sulphate; (c) trace metals such as copper, zinc and iron; (d) buffering agent especially calcium carbonate; and (e) antifoaming agents, e.g. a vegetable oil. Cultivation is at 25 DEG to 35 DEG C., and preferably 28 DEG C., for 1 to 6 days. Compound 616 is recovered from the broth by filtering with a diatomaceous filter aid and then extracting the mycelium cake with an aliphatic alcohol such as methanol, ethanol, propanol, butanol (preferred) or pentanol. The extract is concentrated in vacuo, the precipitated compound 616 resuspended in hexane, filtered and dried. Compound number 616 is an amphoteric polyene compound effective in inhibiting the growth of fungi and containing 62.0% carbon, 7.8% hydrogen, 2.7% nitrogen and 27.5% oxygen; it decomposes at 130-140 DEG C. turning red and then brown; in 0.2% pyridine its specific rotation FORM:0832391/IV (b)/1 aqueous n-propanol its Rf value is 0.72; it is insoluble in water, acetone, methylisopropylketone, methylethylketone, benzene, chloroform, ethyl acetate and methylcyclohexane; soluble in pyridine, dimethylformamide, methanol, ethanol, n - propanol, n - butanol and dioxane; dissolved in 20% aqueous methanol 0.001 N in sodium hydroxide exhibits the following properties in the ultra-violet E1%1 cm.=467 at 340 mm , E1%1 cm.=692 at 358 mm ; E1%1 cm.=959 at 377 mm ; E1%1 cm.=808 at 397 mm ; exhibits characteristic absorption in the infra-red at 3.01, 3.46, 5.88, 6.15, 6.27, 6.37, 7.11, 8.51, 9.40, 9.65, 10.00, 11.83 and 13.18. Compound number 616 forms salt with (a) acids such as sulphuric, hydrochloric, nitric, hydroiodic, hydrobromic, benzenesulphonic, toluenesulphonic, sulphurous and trichloroacetic acids; (b) inorganic bases such as hydroxides and oxides of the alkali and alkaline earth metals, e.g. the sodium, potassium, barium, lithium and calcium salts. Examples illustrate the preparation of the sodium, triethylamine sulphate, hydrochloride and sulphate salts. Compound 616 tends to isomerize in the presence of strong acids, e.g. H2SO4 and p-toluene sulphonic acid and bases. Compound 616 has low phytototoxicity and is used as a plant fungicide (see Group VI).ALSO:An antifungal antibiotic, designated compound number 616, produced by cultivating Streptomyces parvisporogenes ATCC 12568 (see Group IV (b)), has low phytotoxicity and is used in compositions for the treatment of fungal diseases in plants. It may be used in the crude or pure form as such or in the form of a salt such as the sulphate, hydrochloride, hydrobromide, hydroiodide, benzene sulphonate, toluene sulphonate, trichloroacetate, sodium, potassium, barium, lithium and calcium salts. The crude may be the whole fermentation broth, the concentrated broth, the mycelial cake or the crude obtained on extracting the cake with an alcohol such as butanol. The compositions may be in the form of a spray, emulsion or dusting powder containing 0.01 to 95% of the antibiotic. A suitable spray contains 5% aqueous acetone. A dust may be prepared with pyrophilite, bentonite, talc, kaolin or diatomaceous earth. Optional additions are (a) wetting agents, (b) stabilizers, and (c) buffers. The antibiotic may be dissolved or suspended in waxes or resins. The compositions may be used for the treatment of seeds.
机译:通过培养产生产化合物616的副产链霉菌的菌株(例如,产Streptomyces parvisporogenes)生产新的抗生素,称为“化合物编号616”。在水下好氧条件下,在含有碳源和有机氮源的水性营养培养基中,S。parvisporogenes ATCC 12568。 (a)碳的特定来源是糖,例如葡萄糖,淀粉和甘油;(b)氮是酪蛋白,酪蛋白水解物,玉米粉,花生粉,大豆粉,棉籽粉,小麦面筋,乳白蛋白和胰蛋白tone。其他成分是(a)生长物质,例如酵母提取物,酒糟和糖蜜丁醇发酵残留物; (b)矿物盐,例如氯化钠,磷酸钾,硝酸钠和硫酸镁; (c)微量金属,例如铜,锌和铁; (d)缓冲剂,尤其是碳酸钙;和(e)消泡剂,例如植物油。在25℃至35℃,优选28℃下培养1至6天。通过用硅藻土助滤剂过滤从肉汤中回收化合物616,然后用脂族醇如甲醇,乙醇,丙醇,丁醇(优选)或戊醇萃取菌丝体饼。将萃取液真空浓缩,将沉淀的化合物616重悬于己烷中,过滤并干燥。 616号化合物是一种能有效抑制真菌生长的两性多烯化合物,含有62.0%的碳,7.8%的氢,2.7%的氮和27.5%的氧;在130-140℃下分解,先变红,然后变棕色。在0.2%吡啶中,其比旋光度正丙醇水溶液,其Rf值为0.72;不溶于水,丙酮,甲基异丙基酮,甲基乙基酮,苯,氯仿,乙酸乙酯和甲基环己烷;溶于吡啶,二甲基甲酰胺,甲醇,乙醇,正丙醇,正丁醇和二恶烷;溶于20%甲醇的0.001 N氢氧化钠水溶液,在340 mm的紫外线E1%1 cm = 467处,在358 mm的E1%1 cm。= 692中具有以下性能; E1%1 cm。= 959在377 mm; E1%1 cm。= 808在397毫米处;在3.01、3.46、5.88、6.15、6.27、6.37、7.11、8.51、9.40、9.65、10.00、11.83和13.18的红外光谱中显示出特征吸收。 616号化合物与(a)诸如硫酸,盐酸,硝酸,氢碘酸,氢溴酸,苯磺酸,甲苯磺酸,亚硫酸和三氯乙酸的酸形成盐; (b)无机碱,例如碱金属和碱土金属的氢氧化物和氧化物。钠,钾,钡,锂和钙盐。实施例说明了钠,三乙胺硫酸盐,盐酸盐和硫酸盐的制备。化合物616倾向于在强酸,例如强酸的存在下异构化。 H2SO4和对甲苯磺酸及碱。化合物616具有较低的植物毒性,并被用作植物杀菌剂(见第VI组)。用于治疗植物真菌病的组合物中。它可以原样或纯净形式使用,也可以以盐的形式使用,例如硫酸盐,盐酸盐,氢溴酸盐,氢碘酸盐,苯磺酸盐,甲苯磺酸盐,三氯乙酸盐,钠,钾,钡,锂和钙盐。粗产物可以是整个发酵液,浓缩肉汤,菌丝体饼或用醇如丁醇萃取饼得到的粗产物。所述组合物可以是包含0.01至95%的抗生素的喷雾剂,乳剂或撒粉剂的形式。合适的喷雾剂包含5%的丙酮水溶液。可以用硫铁矿,膨润土,滑石,高岭土或硅藻土制备粉尘。可选的添加剂是(a)润湿剂,(b)稳定剂和(c)缓冲剂。抗生素可以溶解或悬浮在蜡或树脂中。该组合物可用于处理种子。

著录项

  • 公开/公告号GB832391A

    专利类型

  • 公开/公告日1960-04-06

    原文格式PDF

  • 申请/专利权人 CHAS. PFIZER & CO. INC.;

    申请/专利号GB19570019284

  • 发明设计人

    申请日1957-06-19

  • 分类号

  • 国家 GB

  • 入库时间 2022-08-23 19:05:08

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