Antiviral activity and synthesis of quaternized promazine derivatives against HSV-1
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- 作者：Akasha K. Purohit ; Matthew D. Balish ; Jacob J. Leichty ; Ashley Roe ; Lori M. Ward ; Miguel O. Mitchell ; Shao-chung Hsia
- 关键词：HSV-1 ; N-(4-Chlorobenzyl)triflupromazinium chloride ; Acyclovir ; Anti-viral ; Structure&ndash ; activity relationship ; Resistance inhibition
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：15 August, 2012
- 年：2012
- 卷：22
- 期：16
- 页码：5308-5312
- 全文大小：644 K
文摘
N-(4-chlorobenzyl)triflupromazinium chloride, a known antitubercular agent, has been found to also be active against HSV-1. A preliminary structure-activity relation has been explored to determine which groups are crucial to viral inhibition. Antiviral assessments such as GFP reduction, plaque reduction, treatment timing and wash-out studies have also been probed to determine a mode of action for QPD-1. Based on this preliminary data, it appears that QPD-1 is a reversible inhibitor, suspected to inhibit early stages of viral replication of HSV-1 at 50 ¦ÌM, equipotent to acyclovir.