CAS: 11011-38-4; 8-Ethyl-5,19-Dihydroxy-3-(1-(4-Hydroxy-3-Methoxycyclohexyl)Prop-1-En-2-yl)-14,16-Dimethoxy-4,10,12,18-Tetramethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26A-Hexadecahydro-3H-15,19-Epoxypyrido[2,1-C][1]Oxa[4]Azacyclotricosine-1,7,20,21(4H,23H)-Tetraone

该化合物是某种大型滑坡抗生素,其特点是,它具有由某些真菌物种发酵而衍生出来的大型抗生素,特别是类动物* 的发酵,它展示了广泛的抗风素活动,主要针对各种真菌感染,对* Candida* 物种和某些霉素特别有效; 食肉动物功能,它抑制了真菌细胞壁的合成,干扰蛋白合成,最终导致细胞死亡; 这种化合物的特点是复杂的分子结构,包括一个大型的乳腺环和多种氢氧基组,有助于其生物活动; 食肉素还因其免疫抑制特性而著名,使其在移植医学领域受到关注; 其溶解于有机溶剂中的溶解性和水溶性有限是显著的物理特性; 由于其强大的效应和特定行动机制,在临床和研究环境中均使用可燃素,尽管其使用可能受到某些病原体的潜在副作用和耐力的限制.

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    专利信息


    专利号:US-9315483-B2
    优先权日:2007-09-13
    标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
    发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
    权利人:CONCERT PHARMACEUTICALS INC
    摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

    专利号:US-6004787-A
    优先权日:1991-01-17
    标题:Method of directing biosynthesis of specific polyketides
    发明人:KATZ LEONARD; DONADIO STEFANO; MCALPINE JAMES B
    权利人:ABBOTT LAB
    摘要:A method to produce novel polyketide structures by designing and introducing specified changes in the DNA governing the synthesis of the polyketide is disclosed. The biosynthesis of specific polyketide analogs is accomplished by genetic manipulation of a polyketide-producing microorganism by isolating a polyketide biosynthetic gene-containing DNA sequence, identifying enzymatic activities associated within the DNA sequence, introducing one or more specified changes into the DNA sequence which codes for one of the enzymatic activities which results in an altered DNA sequence, introducing the altered DNA sequence into the polyketide-producing microorganism to replace the original sequence, growing a culture of the altered microorganism under conditions suitable for the formation of the specific polyketide analog, and isolating the specific polyketide analog from the culture. The method is most useful when the segment of the chromosome modified is involved in an enzymatic activity associated with polyketide biosynthesis, particularly for manipulating polyketide synthase genes from Saccarharopolyspora or Streptomyces.

    专利号:WO-9313663-A1
    优先权日:1992-01-17
    标 题:Method of directing biosynthesis of specific polyketides
    发明人:KATZ LEONARD; DONADIO STEFANO; MCALPINE JAMES B
    权利人:ABBOTT LAB
    摘要:A method to produce novel polyketide structures by designing and introducing specified changes in the DNA governing the synthesis of the polyketide is disclosed. The biosynthesis of specific polyketide analogs is accomplished by genetic manipulation of a polyketide-producing microorganism by isolating a polyketide biosynthetic gene-containing DNA sequence, identifying enzymatic activities associated within the DNA sequence, introducing one or more specified changes into the DNA sequence which codes for one of the enzymatic activities which results in an altered DNA sequence, introducing the altered DNA sequence into the polyketide-producing microorganism to replace the original sequence, growing a culture of the altered microorganism under conditions suitable for the formation of the specific polyketide analog, and isolating the specific polyketide analog from the culture. The method is most useful when the segment of the chromosome modified is involved in an enzymatic activity associated with polyketide biosynthesis, particularly for manipulating polyketide synthase genes from Saccharapolyspora or Streptomyces.

    专利号:EP-0626806-A1
    优先权日:1992-01-17
    标 题 :Method of directing biosynthesis of specific polyketides
    发明人:KATZ LEONARD; DONADIO STEFANO; MCALPINE JAMES B
    权利人:ABBOTT LAB
    摘要:A process for producing new polyketide structures in which predetermined modifications are determined and introduced into the DNA controlling the synthesis of the polyketide. Biosynthesis of specific polyketide analogs is accomplished by modifying a polyketide-producing microorganism by genetic manipulation by isolating a DNA sequence containing a polyketide biosynthetic gene, identifying associated enzymatic activities within the DNA sequence, introducing one or more predetermined modifications in the DNA sequence which encodes one of the enzymatic activities producing a modified DNA sequence, by introducing this modified DNA sequence into the polyketide-producing microorganism in place of the original sequence, by culturing the modified microorganism under conditions suitable for the formation of the specific polyketide analogue, then isolating the specific polyketide analogue from this culture. This method is particularly useful when the modified chromosome segment is involved in enzymatic activity associated with polyketide biosynthesis, more specifically for manipulating polyketide synthase genes from the genus Saccharapolyspora or the genus Streptomyces.

    专利号:US-6437151-B2
    优先权日:1996-07-05
    标题:Erythromycins and process for their preparation
    发明人:LEADLAY PETER FRANCIS; STAUNTON JAMES; CORTES JESUS; PACEY MICHAEL STEPHEN
    权利人:BIOTICA TECH LTD; PFIZER
    摘要:Erythromycins, particularly ones with novel C-13 substituents R1 (e.g. C3-C6 cycloalkyl or cycloalkenyl groups) are prepared by fermenting suitable organisms in the presence of R1CO2H. A preferred organism is Saccharopolyspora erythraea preferably containing an integrated plasmid capable of directing synthesis of desired compounds.

    专利号:WO-2009035652-A1
    优先权日:2007-09-13
    标 题 :Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof

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    合成参考文献


    参考文献:10.7164/antibiotics.50.1036
    摘要:Tanaka Y, Komaki H, Yazawa K, Mikami Y, Nemoto A, Tojyo T, Kadowaki K, Shigemori H, Kobayashi J. Brasilinolide A, a new macrolide antibiotic produced by Nocardia brasiliensis: producing strain, isolation and biological activity. J Antibiot (Tokyo). 1997 Dec;50(12):1036–41. doi: 10.7164/antibiotics.50.1036.
    参考文献:10.7164/antibiotics.41.1592
    摘要:Hatanaka H, Kino T, Miyata S, Inamura N, Kuroda A, Goto T, Tanaka H, Okuhara M. FR-900520 and FR-900523, novel immunosuppressants isolated from a Streptomyces. II. Fermentation, isolation and physico-chemical and biological characteristics. J Antibiot (Tokyo). 1988 Nov;41(11):1592–601. doi: 10.7164/antibiotics.41.1592.
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