CAS: 144348-08-3; (2R,3R,4S,5R)-2-(6-Amino-2-(2-(Cyclohexylmethylene)Hydrazinyl)-9H-Purin-9-yl)-5-(Hydroxymethyl)Tetrahydrofuran-3,4-Diol

该化合物是一种化学修改的代氨基衍生物,具有环己基甲基氢氮基替代成分.这种结构修改增强了其作为生物化学探测器或核糖基研究中间体的潜力.环己基组引入了亲性,这可能比未经过改良的二氧基苯丙胺提高膜渗透性和稳定性.其氢氮基联系为进一步衍生提供了再活动性,使其在合成应用中有用.该化合物对探探探代氨基受体相互作用或酶抑制研究的药用化学具有兴趣.建议由于反应性氢酸混合物的特性而谨慎处理.分析性定性应包括HPLC和质量光谱测量,以确认纯度和特性.

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    专利信息


    专利号:US-2023271983-A1
    优先权日:2020-07-29
    标题 :Functionalized isonitriles and products, preparation and uses thereof
    发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA
    权利人:UNIV SANTIAGO COMPOSTELA
    摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.

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    主要参考文献


    1: Glover DK, Ruiz M, Yang JY, Koplan BA, Allen TR, Smith WH, Watson DD, Barrett RJ, Beller GA. Pharmacological stress thallium scintigraphy with 2-cyclohexylmethylidenehydrazinoadenosine (WRC-0470). A novel, short-acting adenosine A2A receptor agonist. Circulation. 1996 Oct 1;94(7):1726-32. Review. doi: 10.1161/CIRCIMAGING.108.817932. Epub 2009 Sep 17. Epub 2007 Apr 16. Epub 2004 Jan 20. doi: 10.1007/s12350-011-9474-9. Review. doi: 10.1016/j.bbamem.2010.12.017. Epub 2010 Dec 23. Review.
    10: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2004 May;26(4):295-318. Review.
    12: Sullivan GW, Linden J, Buster BL, Scheld WM. Neutrophil A2A adenosine receptor inhibits inflammation in a rat model of meningitis: synergy with the type IV phosphodiesterase inhibitor, rolipram. J Infect Dis. 1999 Nov;180(5):1550-60. Epub 2007 Apr 18. doi: 10.1001/jama.299.18.2140.

    合成参考文献


    摘要:Drug Development Research., 42(76), 1997
    参考文献:10.1016/j.bmc.2012.11.021
    摘要:El-Tayeb A, Gollos S. Synthesis and structure-activity relationships of 2-hydrazinyladenosine derivatives as A(2A) adenosine receptor ligands. Bioorg Med Chem. 2013 Jan 15;21(2):436–47. doi: 10.1016/j.bmc.2012.11.021.
    参考文献:10.1016/j.nuclcard.2006.05.006
    摘要:Cummings M, Raza J, Movahed A. Atrial fibrillation during adenosine pharmacologic stress testing. J Nucl Cardiol. 2006 Jul;13(4):576–81. doi: 10.1016/j.nuclcard.2006.05.006.
    参考文献:10.1016/j.nuclcard.2008.02.013
    摘要:Thomas GS, Tammelin BR, Schiffman GL, Marquez R, Rice DL, Milikien D, Mathur V. Safety of regadenoson, a selective adenosine A2A agonist, in patients with chronic obstructive pulmonary disease: A randomized, double-blind, placebo-controlled trial (RegCOPD trial). Journal of Nuclear Cardiology. 2008 Apr 14;15(3):319–28. doi: 10.1016/j.nuclcard.2008.02.013.
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