CAS: 59865-16-6; Iso Cyclosporin A

该化合物是一种环球浸泡物,是环球甲醚的衍生物,以其免疫抑制特性而著称,主要特征是独特的环状结构,由11种氨酸组成,在特定序列中相连,有助于其生物活动;Isocylosporin A展示了高度的亲眼病性,影响其溶性,影响其生物膜的可溶性和渗透性;该化合物因其能够抑制T细胞的活化和扩散,使其在移植医学和自动免疫疾病治疗中具有价值而引人注目;该作用机制涉及与环球菌结合,导致抑制Calcileurin,这是T细胞信号路径中的一种关键酶.此外,Isocyloosporin A可能与其母体化合物相比具有不同程度的药用性皮肤病特性,影响其治疗效率和安全性特征.与许多免疫抑制剂一样,谨慎的监测对于管理潜在的副作用至关重要,包括增加感染和器官毒性的敏感度.

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cyclosporin A

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    专利信息


    专利号:US-4396542-A
    优先权日:1980-02-14
    标 题 :Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production
    发明人:WENGER ROLAND
    权利人:SANDOZ LTD
    摘要:A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.

    专利号:US-4554351-A
    优先权日:1980-02-14
    标 题:Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production
    发明人:WENGER ROLAND
    权利人:SANDOZ LTD
    摘要:A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.

    专利号:CN-1571795-A
    优先权日:2001-10-19
    标 题:Synthesis of Cyclosporine Analogs

    专利号:EP-0034567-B1
    优先权日:1980-02-14
    标 题 :A method for the total synthesis of cyclosporins and novel cyclosporins

    专利号:EP-0098457-B1
    优先权日:1980-02-14
    标 题:(1s,2r,3r)- and (1r,2s,3s)-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes useful in the total synthesis of cyclosporins and processes for their production

    专利号:IE-54936-B1
    优先权日:1980-02-14
    标 题:A method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Sanglier JJ, Traber R, Buck RH, Hofmann H, Kobel H. Isolation of (4R)-4-[(E)-2-butenyl]-4-methyl-L-threonine, the characteristic structural element of cyclosporins, from a blocked mutant of Tolypocladium inflatum. J Antibiot (Tokyo). 1990 Jun;43(6):707-14.

    合成参考文献


    参考文献:10.1021/acs.jmedchem.8b01259
    摘要:Naylor MR, Ly AM, Handford MJ, Ramos DP, Pye CR, Furukawa A, Klein VG, Noland RP, Edmondson Q, Turmon AC, Hewitt WM, Schwochert J, Townsend CE, Kelly CN, Blanco MJ, Lokey RS. Lipophilic Permeability Efficiency Reconciles the Opposing Roles of Lipophilicity in Membrane Permeability and Aqueous Solubility. J Med Chem. 2018 Dec 27;61(24):11169–82. doi: 10.1021/acs.jmedchem.8b01259.
    参考文献:10.1021/acs.jmedchem.1c00580
    摘要:Corbett KM, Ford L, Warren DB, Pouton CW, Chalmers DK. Cyclosporin Structure and Permeability: From A to Z and Beyond. J Med Chem. 2021 Sep 23;64(18):13131–51. doi: 10.1021/acs.jmedchem.1c00580.
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