CAS: 103476-89-7; (S)-2-Acetamido-N-((S)-1-(((S)-5-Guanidino-1-Oxopentan-2-yl)Amino)-4-Methyl-1-Oxopentan-2-yl)-4-Methylpentanamide Hemisulfate

该化合物是一种复杂的有机化合物,其结构成分特征包括氨酸衍生物(L-lecine)和硫酸组.该化合物具有独特的功能组安排,包括有助于其生物活动和溶性特性的氨基和丙基功能.硫酸混合物的存在会增强其营养特性,有可能影响其与生物系统的互动和在水生环境中的溶性.作为L-leucine的衍生物,它可能表现出与蛋白合成和代谢相关的特性.该化合物的立体化学学,特别是(1S)配置,表明可影响其生物相互作用的具体空间安排.

结构式图片

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合成工艺路线路线简述

    专利信息


    专利号:WO-9312076-A1
    优先权日:1991-12-13
    标题:Reagents for automated synthesis of peptide analogs
    发明人:WEBB THOMAS ROY
    权利人:CORVAS INT INC
    摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.

    专利号:US-7169589-B2
    优先权日:2000-07-28
    标题 :Silicatein-mediated synthesis of amorphous silicates and siloxanes and use thereof
    发明人:MUELLER WERNER E G; SCHROEDER HEINZ C; LORENZ BERND; KRASKO ANATOLI
    权利人:MUELLER WERNER E G; SCHROEDER HEINZ C; LORENZ BERND; KRASKO ANATOLI
    摘要:Silicatein is an enzyme of silicate-forming organisms used for the synthesis of their silicate scaffold. The present invention relates to the use of highly-expressed and highly active recombinant silicatein, silicatein isolated from natural sources after gene induction as well as silicatein-fusion proteins for the synthesis of amorphous silicon dioxide (silicic acids and silicates), siloxanes as well as modification of these compounds and their technical use.

    专利号:US-5283293-A
    优先权日:1990-12-14
    标 题:Reagents for automated synthesis of peptide analogs
    发明人:WEBB THOMAS R
    权利人:CORVAS INC
    摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.

    专利号:US-5367072-A
    优先权日:1990-12-14
    标 题 :Reagents for automated synthesis of peptide analogs
    发明人:WEBB THOMAS R
    权利人:CORVAS INT INC
    摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.

    专利号:EP-0790982-B1
    优先权日:1994-06-17
    标 题 :Methods of synthesis of peptidyl argininals
    发明人:WEBB THOMAS R; REINER JOHN E; TAMURA SUSAN Y; RIPKA WILLIAM C; DAGNINO RAYMOND JR; NUTT RUTH F
    权利人:CORVAS INT INC
    摘要:This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to novel reagents useful therein, which have formula (I), wherein R1 is selected from the group consisting of hydrogen, benzyloxycarbonyl, isonicotinyloxycarbonyl, 2-chlorobenzyloxycarbonyl, 4-methoxybenzyloxycarbonyl, t-butoxycarbonyl, t-amyloxycarbonyl, isobornyloxycarbonyl, adamantyloxycarbonyl, 2-(4-biphenyl)-2-propyloxycarbonyl, 9-fluorenylmethoxycarbonyl and methylsulfonylethoxycarbonyl; R2 is selected from the group consisting of alkyl of 1 to about 12 carbon atoms and aralkyl of about 7 to about 15 carbon atoms, either of which is optionally substituted with hydroxy or -CO-Y, wherein Y is hydroxy, alkoxy of 1 to about 12 carbon atoms, aralkoxy of about 7 to about 15 carbon atoms, O-polymeric support or NH-polymeric support; R3 is selected from the group consisting of hydrogen, Fmoc, nitro, benzyloxycarbonyl, t-butoxycarbonyl and adamantyloxycarbonyl; and R4 is selected from the group consisting of hydrogen, alkyl of 1 to about 12 carbon atoms, aryl of about 6 to about 14 carbon atoms and aralkyl of about 7 to about 15 carbon atoms; and salts thereof.

    专利号:US-5731413-A
    优先权日:1994-06-17
    标 题:Method of synthesis of peptidyl aldehydes
    发明人:WEBB THOMAS ROY; REINER JOHN EUGENE; TAMURA SUSAN YOSHIKO; RIPKA WILLIAM CHARLES; DAGNINO JR RAYMOND; NUTT RUTH FOELSCHE
    权利人:CORVAS INT INC
    摘要:This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to novel! reagents useful therein.
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    主要参考文献


    1: Hashimoto Y. Gelatin Zymography Using Leupeptin for the Detection of Various Cathepsin L Forms. Methods Mol Biol. 2017;1594:243-254. doi: 10.1007/978-1-4939-6934-0_16. 83(6):2566-74. doi: 10.1128/IAI.02966-14. Epub 2015 Apr 13.
    3: Childers MK, Bogan JR, Bogan DJ, Greiner H, Holder M, Grange RW, Kornegay JN. Chronic administration of a leupeptin-derived calpain inhibitor fails to ameliorate severe muscle pathology in a canine model of duchenne muscular dystrophy. Front Pharmacol. 2012 Jan 9;2:89. doi: 10.3389/fphar.2011.00089.
    4: Gavriel H, Shulman A, Stracher A, Sohmer H. Leupeptin reduces impulse noise induced hearing loss. J Occup Med Toxicol. 2011 Dec 29;6:38. doi: 10.1186/1745-6673-6-38.

    合成参考文献


    参考文献:10.1515/bc.2006.091
    摘要:Kishi T, Cloutier SM, Kündig C, Deperthes D, Diamandis EP. Activation and enzymatic characterization of recombinant human kallikrein 8. Biol Chem. 2006 Jun;387(6):723–31. doi: 10.1515/bc.2006.091.
    参考文献:10.1016/0014-5793(93)80557-b
    摘要:Sarubbi E, Seneci PF, Angelastro MR, Peet NP, Denaro M, Islam K. Peptide aldehydes as inhibitors of HIV protease. FEBS Lett. 1993 Mar 22;319(3):253–6. doi: 10.1016/0014-5793(93)80557-b.
    参考文献:10.1016/j.bmc.2014.05.037
    摘要:Raghav N, Singh M. SAR studies of differently functionalized chalcones based hydrazones and their cyclized derivatives as inhibitors of mammalian cathepsin B and cathepsin H. Bioorg Med Chem. 2014 Aug 01;22(15):4233–45. doi: 10.1016/j.bmc.2014.05.037.
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