CAS: 124436-59-5; Ethyl 4-(2-(1-(6-Methylpyridazin-3-yl)Piperidin-4-yl)Ethoxy)Benzoate

该化合物是一种抗病毒化合物,主要因其在治疗病毒感染方面的潜力而受到调查,尤其是由造成普通寒冷的犀牛病毒造成的病毒感染,属于类似天然核素类比的化合物,它模仿天然核素类比的结构,干扰病毒复制. Pirodavir展示了一种行动机制,它涉及抑制病毒性RNA合成,从而防止病毒在宿主细胞中繁殖.该物质的特点是其分子重量相对较低,并且有特定功能组群,有助于其抗病毒活动.在溶液方面,Pirodavir通常在各种溶剂中进行评估,以确定其生物利用率和药用基因特性.尽管它在临床学研究中表现出希望,但进一步研究对于充分了解其功效,安全性以及临床环境中的潜在治疗应用来说是必要的.与许多抗病毒剂一样,抗药性的发展以及混合疗法的需要是其使用中的重要考虑因素.

结构式图片

上下游产品

Ethyl 4-hydroxybenzoate 3-methyl-6-[4-(2-chloroethyl)-1-piperidynyl]pyridazine

合成工艺路线路线简述

    📜过氧化氢酶,3-[4-(2-氯乙基)-1-哌啶基]-6-甲基哒嗪置于potassium Carbonate体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应生成吡罗达韦
    参考文献:An Orally Bioavailable Oxime Ether Capsid Binder With Potent Activity Against Human Rhinovirus
    标题:An Orally Bioavailable Oxime Ether Capsid Binder With Potent Activity Against Human Rhinovirus
    摘要:A Series Of Capsid-Binding Compounds Was Screened Against Human Rhinovirus (Hrv) Using A Cpe Based Assay. The Ethyl Oxime Ether 14 Was Found To Have Outstanding Anti-Hrv Activity (Median Ic50 4.75 Ng/ml),And Unlike The Equivalent Ethyl Ester Compound 3 (Pirodavir),It Has Good Oral Bioavailability,Making It A Promising Development Candidate. Compound 14 Illustrates That An Oxime Ether Group Can Act As A Metabolically Stable Bioisostere For An Ester Functionality.
    Doi:10.1021/jm0202876

    海关参考信息

    专利信息


    专利号:US-2022233673-A1
    优先权日:2019-06-04
    标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
    发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
    权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
    摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

    专利号:US-6534530-B1
    优先权日:1999-08-04
    标题:Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
    发明人:DRAGOVICH PETER SCOTT; ZHOU RU; WEBBER STEPHEN EVAN; PRINS THOMAS J; REICH SIEGFRIED HEINZ; KEPHART SUSAN E; RUI YUANJIN
    权利人:AGOURON PHARMA
    摘要:Compounds of the formula:where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.

    专利号:WO-2009056955-A1
    优先权日:2007-10-30
    标题 :Amine-bearing phospholipids (abps), their synthesis and use
    发明人:ZUMBUEHL ANDREAS
    权利人:UNIV BASEL; ZUMBUEHL ANDREAS
    摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.

    专利号:WO-2009016425-A1
    优先权日:2007-08-02
    标题 :Compounds of chemical synthesis with antirhinovirus activity
    发明人:POMPEI RAFFAELLO; TARRO GIULIO
    权利人:UNIHART CORP
    摘要:The present invention relates to a lead compound UBP 502 with the formula ethyl -4- (5- (S-methylisoxazol-5-ylamino)pentyloxy)benzoate, and to a series of its analogs. UBP 502, compared to the reference compound R 77975 (Pirodavir) from the formula ethyl-4-(2-(l-(6-methylpirazine-3-iI)-43 pyperidil)etqxy benzoate presents, in vitro, a lesser cytpxicity combined with an adequate therapeutic index to envisage the potential clinical application. Moreover, when administered for oral route resulted to be bioavailable and metabolically stable compared to R 77975.

    专利号:US-10092587-B2
    优先权日:2014-06-25
    标题:Antiviral composition containing material involved in phosphatidylcholine synthesis pathway
    发明人:KWON DUR HAN; JANG MI JIN; SONG JAE HYOUNG; ENKHTAIVAN GANSUKH; OH SEI RYANG
    权利人:KOREA RES INST BIOSCIENCE & BIOTECHNOLOGY
    摘要:The present invention relates to an antiviral composition comprising any one selected from the group consisting of chlorine, phosphocholine, cytidine triphosphate, CDP-choline, phosphorylcholine, and phosphatidylcholine. The antiviral composition is harmless to the human body and exhibits an excellent inhibitory effect on virus proliferation. Therefore, it can be applied to a pharmaceutical composition for preventing or treating viral diseases as well as a health functional food, a quasi-drug composition, and a feed composition for preventing or ameliorating viral diseases.

    专利号:US-9907753-B2
    优先权日:2010-03-19
    标 题 :Lipid vesicle compositions and methods of use
    发明人:IRVINE DARRELL J; MOON JAEHYUN
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:The invention provides delivery systems comprised of stabilized multilamellar vesicles, as well as compositions, methods of synthesis, and methods of use thereof. The stabilized multilamellar vesicles may comprise prophylactic, therapeutic and/or diagnostic agents.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Tang Q, Xu Z, Zhang F, Cai Y, Chen Y, Lu B, Zhou HB, Lan K, Wu S. Identification of a novel binding inhibitor that blocks the interaction between hSCARB2 and VP1 of enterovirus 71. Cell Insight. 2022 Feb 12;1(2):100016. doi: 10.1016/j.cellin.2022.100016.
    2: Lanko K, Shi C, Patil S, Delang L, Matthijnssens J, Mirabelli C, Neyts J. Assessing In Vitro Resistance Development in Enterovirus A71 in the Context of Combination Antiviral Treatment. ACS Infect Dis. 2021 Oct 8;7(10):2801-2806. doi: 10.1021/acsinfecdis.0c00872. Epub 2021 Sep 16. 31(4):479-489. doi: 10.1007/s13337-020-00631-w. Epub 2020 Nov 11.
    4: Wang Y, Wang H, Jiang X, Jiang Z, Guo T, Ji X, Li Y, Li Y, Li Z. Synthesis and Broad Antiviral Activity of Novel 2-aryl-isoindolin-1-ones towards Diverse Enterovirus A71 Clinical Isolates. Molecules. 2019 Mar 11;24(5):985. doi: 10.3390/molecules24050985.

    合成参考文献


    摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198
    参考文献:10.1128/aac.36.4.727
    摘要:Hayden FG, Andries K, Janssen PA. Safety and efficacy of intranasal pirodavir (R77975) in experimental rhinovirus infection. Antimicrob Agents Chemother. 1992 Apr;36(4):727–32.
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