Exploration of a new series of CCR5 antagonists: multi-dimensional optimization of a sub-series containing N-substituted pyrazoles.

Lemoine RC; Petersen AC; Setti L; Jekle A; Heilek G; deRosier A; Ji C; Berry P; Rotstein DM

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Exploration of a new series of CCR5 antagonists: multi-dimensional optimization of a sub-series containing N-substituted pyrazoles.

机译：探索一系列新的CCR5拮抗剂：多维优化包含N-取代的吡唑的子系列。

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The introduction of N-substituted pyrazoles in a new series of CCR5 antagonists was shown to substantially increase antiviral activity.

机译：N取代的吡唑类化合物在一系列新的CCR5拮抗剂中的引入可显着提高抗病毒活性。

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《Bioorganic and Medicinal Chemistry Letters 》 |2010年第16期| 共4页
作者
Lemoine RC; Petersen AC; Setti L; Jekle A; Heilek G; deRosier A; Ji C; Berry P; Rotstein DM;
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1. Exploration of a new series of CCR5 antagonists: multi-dimensional optimization of a sub-series containing N-substituted pyrazoles. [J] . Lemoine RC, Petersen AC, Setti L, Bioorganic and Medicinal Chemistry Letters . 2010 ,第16期

机译：探索新系列CCR5拮抗剂：含N-取代吡唑的子系列的多维优化。
2. Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles. [J] . Lemoine RC, Petersen AC, Setti Bioorganic and Medicinal Chemistry Letters . 2010 ,第2期

机译：评估一系列CCR5拮抗剂中的仲酰胺替代物，以增加固有膜通透性。第1部分：宝石二取代氮杂环的优化。
3. Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series. [J] . Wanner J, Chen L, Lemoine RC, Bioorganic and Medicinal Chemistry Letters . 2010 ,第22期

机译：评价CCR5拮抗剂中的酰胺替代物，以增加内在渗透性。第2部分：同源氮杂系列的SAR优化和药代动力学概况。
4. Study on CCR5 Receptor Antagonists as an Anti-Prostate Cancer: Inhibition Activity, QSAR and Molecular Docking [C] . Nursamsiar, Lina Nurfadhila, Iman S. Pratama, International Conference on Computation for Science and Technology . 2015

机译：CCR5受体拮抗剂作为抗前列腺癌的研究：抑制活性，QSAR和分子对接
5. Do CCR5 Antagonists Have a Role in Inflammatory Disorders? [D] . Naqvi, Syed Azim. 2019

机译：CCR5拮抗剂是否在炎症障碍中作用？
6. Pharmacokinetics and Pharmacodynamics of TBR-652 a Novel CCR5 Antagonist in HIV-1-Infected Antiretroviral Treatment-Experienced CCR5 Antagonist-Naïve Patients [O] . Jean-Francois Marier, MyMy Trinh, Leng Hong Pheng, 2011

机译：新型CCR5拮抗剂TBR-652在未经HIV-1感染抗逆转录病毒治疗的CCR5初治患者中的药代动力学和药效学
7. Pharmacokinetics and Pharmacodynamics of TBR-652, a Novel CCR5 Antagonist, in HIV-1-Infected, Antiretroviral Treatment-Experienced, CCR5 Antagonist-Naïve Patients▿† [O] . Marier, Jean-Francois, Trinh, MyMy, Pheng, Leng Hong, 2011

机译：TBR-652（一种新型CCR5拮抗剂）在受HIV-1感染，抗逆转录病毒治疗且没有CCR5拮抗剂的患者中的药代动力学和药效动力学dynamic†

Exploration of a new series of CCR5 antagonists: multi-dimensional optimization of a sub-series containing N-substituted pyrazoles.

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