Antiviral activity and synthesis of quaternized promazine derivatives against HSV-1.
Antiviral activity and synthesis of quaternized promazine derivatives against HSV-1.
复制标题
针对 HSV-1 的季铵化丙嗪衍生物的抗病毒活性和合成。
DOI：
10.1016/j.bmcl.2012.06.031
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发表时间：
2012
影响因子：
2.7
通讯作者：
Hsia,Shao-chung
中科院分区：
文献类型：
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作者：
Purohit,AkashaK;Balish,MatthewD;Leichty,JacobJ;Roe,Ashley;Ward,LoriM;Mitchell,MiguelO;Hsia,Shao-chung
已知的抗结核药N-（4-氯苄基）三氟丙嗪鎓氯化物也被发现对HSV-1有活性。已探索了初步的结构-活性关系，以确定哪些基团对病毒抑制至关重要。还探索了抗病毒评估，如GFP减少、空斑减少、治疗时机和洗脱研究，以确定QPD-1的作用模式。基于该初步数据，QPD-1似乎是一种可逆抑制剂，怀疑在50μM时抑制HSV-1病毒复制的早期阶段，与阿昔洛韦等效。
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 50μM, equipotent to acyclovir.