898264-60-3Relevant academic research and scientific papers
KETOAMIDE COMPOUND AND PREPARATION METHOD, PHARMACEUTICAL COMPOSITION, AND USE THEREOF
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Paragraph 0098; 0102, (2021/06/21)
A ketoamide compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically, the ketoamide compound shown in formula (A), a racemate, an enantiomer, or a diastereoisomer thereof, or any mixture of same, or a pharmaceutical
Inhibitors of cysteine proteases and methods of use thereof
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Page/Page column 416-418; 454-456, (2021/09/22)
The disclosure provides compounds with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease. Exemplary compounds provided include Formula II-I, where R3, RB are provided herein:
Synthesis, crystal structure, structure-activity relationships, and antiviral activity of a potent SARS coronavirus 3CL protease inhibitor
Yang, Syaulan,Chen, Shu-Jen,Hsu, Min-Feng,Wu, Jen-Dar,Tseng, Chien-Te K.,Liu, Yu-Fan,Chen, Hua-Chien,Kuo, Chun-Wei,Wu, Chi-Shen,Chang, Li-Wen,Chen, Wen-Chang,Liao, Shao-Ying,Chang, Teng-Yuan,Hung, Hsin-Hui,Shr, Hui-Lin,Liu, Cheng-Yuan,Huang, Yu-An,Chang, Ling-Yin,Hsu, Jen-Chi,Peters, Clarence J.,Wang, Andrew H.-J.,Hsu, Ming-Chu
, p. 4971 - 4980 (2007/10/03)
A potent SARS coronavirus (CoV) 3CL protease inhibitor (TG-0205221, K i = 53 nM) has been developed. TG-0205221 showed remarkable activity against SARS CoV and human coronavirus (HCoV) 229E replications by reducing the viral titer by 4.7 log (at 5 μM) for SARS CoV and 5.2 log (at 1.25 μM) for HCoV 229E. The crystal structure of TG-0205221 (resolution = 1.93 A?) has revealed a unique binding mode comprising a covalent bond, hydrogen bonds, and numerous hydrophobic interactions. Structural comparisons between TG-0205221 and a natural peptide substrate were also discussed. This information may be applied toward the design of other 3CL protease inhibitors.
