CAS: 67879-58-7; (2R,3R)-2-(((E)-3-(3,4-Dihydroxyphenyl)Acryloyl)Oxy)-3-Hydroxysuccinic Acid

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CAS号87-69-4 酒石酸 | CAS号331-39-5 咖啡酸

📜Bis(Diphenylmethyl) 2-(3,4-Di(Tert-Butyldimethylsilyloxy)Cinnamoyl)-3-Hydroxy-L-Tartrate置于溶剂黄146体系中,化学反应 10.0H,以96%的收率获得产物咖啡酰酒石酸
参考文献:Design,Synthesis,And Biological Evaluation Of Novel Hybrid Dicaffeoyltartaric/diketo Acid And Tetrazole-Substituted L-Chicoric Acid Analogue Inhibitors Of Human Immunodeficiency Virus Type 1 Integrase
标题:Design,Synthesis,And Biological Evaluation Of Novel Hybrid Dicaffeoyltartaric/diketo Acid And Tetrazole-Substituted L-Chicoric Acid Analogue Inhibitors Of Human Immunodeficiency Virus Type 1 Integrase
摘要:Fourteen Analogues Of The Anti-Hiv-1 Integrase (In) Inhibitor L-Chicoric Acid (L-Ca) Were Prepared. Their Ic50 Values For 3'-End Processing And Strand Transfer Against Recombinant Hiv-1 In Were Determined In Vitro,And Their Cell Toxicities And Ec50 Against Hiv-1 Were Measured In Cells (Ex Vivo). Compounds 1-6 Are Catechol/beta-Diketoacid Hybrids,The Majority Of Which Exhibit Submicromolar Potency Against 3'-End Processing And Strand Transfer,Though Only With Modest Antiviral Activities. Compounds 7-10 Are L-Ca/p-Fluorobenzylpyrroloyl Hybrids,Several Of Which Were More Potent Against Strand Transfer Than 3'-End Processing,A Phenomenon Previously Attributed To The Beta-Diketo Acid Pharmacophore. Compounds 11-14 Are Tetrazole Bioisosteres Of L-Ca And Its Analogues,Whose In Vitro Potencies Were Comparable To L-Ca But With Enhanced Antiviral Potency. The Trihydroxyphenyl Analogue 14 Was 30-Fold More Potent Than L-Ca At Relatively Nontoxic Concentrations. These Data Indicate That L-Ca Analogues Are Attractive Candidates For Development Into Clinically Relevant Inhibitors Of Hiv-1 In.
DOI:10.1021/jm1010594

专利信息

专利号:US-2025231101-A1
优先权日:2024-01-11
标 题 :Validation of natural matrices for therapeutic use on humans, animals and plants on bio-physical bases as an alternative to validation through chemically definable substances derived from said matrices by isolation and/or synthesis processes and also as an alternative to products comprising natural matrices validated on the basis of their traditional use
发明人：MERCATI VALENTINO; LUCCI JACOPO
权利人:BIOS THERAPY PHYSIOLOGICAL SYSTEMS FOR HEALTH S P A
摘要:The present invention relates to a new method for assessing acceptability ranges or cut-offs for the compliance validation of batches of products comprising or consisting of one or more natural matrix, wherein said products have an ascertained therapeutic or beneficial effect. The invention also relates to a new process for the compliance validation of one or more batches of said products.

专利号:CN-116716335-A
优先权日:2023-05-31
标 题:Application of dandelion TmABI5 gene in promoting plant synthesis of chicoric acid