Design, synthesis & structure-activity relationships of a new class of antihuman enterovirus D68 & A71 agents

Bidyadhar Sethy; Chung Fan Hsieh; Chieh Yeh; Jim Tong Horng; Pei Wen Hsieh

doi:10.4155/fmc-2017-0268

Design, synthesis & structure-activity relationships of a new class of antihuman enterovirus D68 & A71 agents

Bidyadhar Sethy, Chung Fan Hsieh, Chieh Yeh, Jim Tong Horng, Pei Wen Hsieh^*

^*此作品的通信作者

Chang Gung University

研究成果: 期刊稿件 › 文章 › 同行評審

1 引文斯高帕斯（Scopus）

摘要

Aim: No antiviral medications are currently approved to treat enterovirus (EV)-associated disease or prevent EV infection. Methods: In this study, a series of probenecid derivatives were designed via a rational strategy and synthesized to obtain more potent anti-EV agents. Results: Compounds 8 and 24 exhibited the most potent activity against EV D68 and A71, with half maximal effective concentration (EC ₅₀ ) values of 2.49/2.09 and 2.59/2.41 μM, respectively, and revealed a broad inhibition spectrum toward other EV strains, with high selectivity indices. Additionally, compounds 8 and 24 showed good stability in rat serum, with half-lives of 48.39 and 60.26 min, respectively. Conclusion: Compounds 8 and 24 are the promising candidates for the development of new agents against EV D68 and A71 viruses.

原文	英語
頁（從 - 到）	1333-1347
頁數	15
期刊	Future Medicinal Chemistry
卷	10
發行號	11
DOIs	https://doi.org/10.4155/fmc-2017-0268
出版狀態	已出版 - 06 2018

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Publisher Copyright:
© 2018 Newlands Press.

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title = "Design, synthesis & structure-activity relationships of a new class of antihuman enterovirus D68 & A71 agents",

abstract = " Aim: No antiviral medications are currently approved to treat enterovirus (EV)-associated disease or prevent EV infection. Methods: In this study, a series of probenecid derivatives were designed via a rational strategy and synthesized to obtain more potent anti-EV agents. Results: Compounds 8 and 24 exhibited the most potent activity against EV D68 and A71, with half maximal effective concentration (EC 50 ) values of 2.49/2.09 and 2.59/2.41 μM, respectively, and revealed a broad inhibition spectrum toward other EV strains, with high selectivity indices. Additionally, compounds 8 and 24 showed good stability in rat serum, with half-lives of 48.39 and 60.26 min, respectively. Conclusion: Compounds 8 and 24 are the promising candidates for the development of new agents against EV D68 and A71 viruses.",

keywords = "EV A71, EV D68, metabolic stability, optimization, probenecid derivatives",

author = "Bidyadhar Sethy and Hsieh, {Chung Fan} and Chieh Yeh and Horng, {Jim Tong} and Hsieh, {Pei Wen}",

note = "Publisher Copyright: {\textcopyright} 2018 Newlands Press.",

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doi = "10.4155/fmc-2017-0268",

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AU - Sethy, Bidyadhar

AU - Hsieh, Chung Fan

AU - Yeh, Chieh

AU - Horng, Jim Tong

AU - Hsieh, Pei Wen

PY - 2018/6

Y1 - 2018/6

N2 - Aim: No antiviral medications are currently approved to treat enterovirus (EV)-associated disease or prevent EV infection. Methods: In this study, a series of probenecid derivatives were designed via a rational strategy and synthesized to obtain more potent anti-EV agents. Results: Compounds 8 and 24 exhibited the most potent activity against EV D68 and A71, with half maximal effective concentration (EC 50 ) values of 2.49/2.09 and 2.59/2.41 μM, respectively, and revealed a broad inhibition spectrum toward other EV strains, with high selectivity indices. Additionally, compounds 8 and 24 showed good stability in rat serum, with half-lives of 48.39 and 60.26 min, respectively. Conclusion: Compounds 8 and 24 are the promising candidates for the development of new agents against EV D68 and A71 viruses.

AB - Aim: No antiviral medications are currently approved to treat enterovirus (EV)-associated disease or prevent EV infection. Methods: In this study, a series of probenecid derivatives were designed via a rational strategy and synthesized to obtain more potent anti-EV agents. Results: Compounds 8 and 24 exhibited the most potent activity against EV D68 and A71, with half maximal effective concentration (EC 50 ) values of 2.49/2.09 and 2.59/2.41 μM, respectively, and revealed a broad inhibition spectrum toward other EV strains, with high selectivity indices. Additionally, compounds 8 and 24 showed good stability in rat serum, with half-lives of 48.39 and 60.26 min, respectively. Conclusion: Compounds 8 and 24 are the promising candidates for the development of new agents against EV D68 and A71 viruses.

KW - EV A71

KW - EV D68

KW - metabolic stability

KW - optimization

KW - probenecid derivatives

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Design, synthesis & structure-activity relationships of a new class of antihuman enterovirus D68 & A71 agents

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