840490-23-5Relevant academic research and scientific papers
Substituted imidazole formate type derivative and application thereof
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Paragraph 0621; 0622; 0626; 0627; 0628, (2019/06/05)
The invention discloses a compound shown as a formula I or a stereoisomer thereof or pharmaceutically acceptable salts thereof or a solvate thereof or a prodrug thereof or a metabolic product thereofor a deuterated derivative thereof. The compound is a substituted imidazole formate type derivative with a novel structure and belongs to the field of pharmaceutical chemistry. The invention further discloses application of the substituted imidazole formate type derivative to preparation of drugs with calming, hypnosis and/or anesthetic effects and application of the substituted imidazole formatetype derivative to preparation of drugs capable of controlling status epilepticus. The compound disclosed by the invention has a relatively good inhibition effect on a central nervous system and provides a new choice for clinically screening and/or preparing the drugs with the calming, hypnosis and/or anesthetic effects and capable of controlling the status epilepticus. The formula I is shown in the description.
Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase
Chong, Pek,Sebahar, Paul,Youngman, Michael,Garrido, Dulce,Zhang, Huichang,Stewart, Eugene L.,Nolte, Robert T.,Wang, Liping,Ferris, Robert G.,Edelstein, Mark,Weaver, Kurt,Mathis, Amanda,Peat, Andrew
supporting information, p. 10601 - 10609 (2013/02/23)
A new series of non-nucleoside reverse transcriptase inhibitors based on an imidazole-amide biarylether scaffold has been identified and shown to possess potent antiviral activity against HIV-1, including the NNRTI-resistant Y188L mutated virus. X-ray crystallography of inhibitors bound to reverse transcriptase, including a structure of the Y188L RT protein, was used extensively to help identify and optimize the key hydrogen-bonding motif. This led directly to the design of compound 43 that exhibits remarkable antiviral activity (EC50 1 nM) against a wide range of NNRTI-resistant viruses and a favorable pharmacokinetic profile across multiple species.
