Antiviral activity and synthesis of quaternized promazine derivatives against HSV-1.
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 μM, equipotent to acyclovir.
Salisbury University, 1101 Camden Ave., Salisbury, MD 21801, USA.
Akasha K
AK
Purohit
Matthew D
MD
Balish
Jacob J
JJ
Leichty
Ashley
A
Roe
Lori M
LM
Ward
Miguel O
MO
Mitchell
Shao-chung
SC
Hsia
D000212:Acyclovir / Q000494:pharmacology; D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002522:Chlorocebus aethiops; D018259:Herpesvirus 1, Human / Q000187:drug effects*; D006801:Humans; D010640:Phenothiazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011395:Promazine / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000644:Quaternary Ammonium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014709:Vero Cells; D014779:Virus Replication / Q000187:drug effects
D000998:Antiviral Agents; C576478:N-(4-chlorobenzyl)-N,N-dimethyl-2-(2-(trifluoromethyl)-10H-phenothiazin-10-yl) ethanaminium; D010640:Phenothiazines; D000644:Quaternary Ammonium Compounds; D011395:Promazine; D000212:Acyclovir