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Novel benzimidazo[2,1-c][1,4]thiazinone derivatives with potent activity against HSV-1
Journal article   Peer reviewed

Novel benzimidazo[2,1-c][1,4]thiazinone derivatives with potent activity against HSV-1

Shadia A Galal, Shweekar I El-Naem, Ahmed O H El-Nezhawy, Mohamed A Ali and Hoda I El-Diwani
Archiv der Pharmazie (Weinheim), Vol.344(4), pp.255-263
04/2011
DOI: https://doi.org/10.1002/ardp.201000252
PMID: 21469175

Abstract

Animals Antiviral Agents - chemical synthesis Antiviral Agents - chemistry Antiviral Agents - pharmacology Benzimidazoles - chemical synthesis Benzimidazoles - chemistry Benzimidazoles - pharmacology Cell Culture Techniques Cercopithecus aethiops Dose-Response Relationship, Drug Hep G2 Cells Herpesvirus 1, Human - drug effects Herpesvirus 1, Human - growth & development Humans Molecular Structure Thiazines - chemical synthesis Thiazines - chemistry Thiazines - pharmacology Vero Cells
The synthesis of new 2-carboxymethylsulfanylmethyl-1H-benzimidazole and 1,3-dihydro-4H-benzo[4',5']imidazo[2,1-c][1,4]thiazine-4-one-8-carboxylic acid derivatives was investigated. The antiviral activity of compounds 1-14 was tested against the herpes simplex virus 1. Compounds 5 and 14 showed potent activity as they inhibited virus propagation by 94.7% and 91.3% at a dose of 50 µg, respectively. Compounds 5 and 14 showed higher potency than Acyclovir at doses of 20 µg and 50 µg.

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