Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents
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چکیده
منابع مشابه
Structure Optimization of Neuraminidase Inhibitors as Potential Anti-influenza (H1N1Inhibitors) Agents Using QSAR and Molecular Docking Studies
The urgent need of neuraminidase inhibitors (NI) has provided an impetus for understanding the structure requisite at molecular level. Our search for selective inhibitors of neuraminidase has led to the identification of pharmacophoric requirements at various positions around acyl thiourea pharmacophore. The main objective of present study is to develop selective NI, with least toxicity and dru...
متن کاملStructure Optimization of Neuraminidase Inhibitors as Potential Anti-influenza (H1N1Inhibitors) Agents Using QSAR and Molecular Docking Studies
The urgent need of neuraminidase inhibitors (NI) has provided an impetus for understanding the structure requisite at molecular level. Our search for selective inhibitors of neuraminidase has led to the identification of pharmacophoric requirements at various positions around acyl thiourea pharmacophore. The main objective of present study is to develop selective NI, with least toxicity and dru...
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Influenza virus neuraminidase (NA) catalyses the cleavage of sialic acid residues terminally linked to glycoproteins and glycolipids and plays an important role in the replication of the virus. Recently, several potent NA inhibitors have been synthesized based on the rational design of mimicking the transition state of the sialic acid cleavage. Zanamivir and oseltamivir (GS 4104, the prodrug of...
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Introduction: The emergence and spread of the pandemic H1N1 influenza virus in 2009 indicates a limitation in the strategy to control the infection, despite a long-established vaccination programme and approved antivirals. Production the proper vaccine against influenza is difficult due to the genetic recombination of virus in the event of pandemic and co-circulation of drug-resistance variants...
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We report the synthesis and antimalarial activities of eighteen quinoxaline and quinoxaline 1,4-di-N-oxide derivatives, eight of which are completely novel. Compounds 1a and 2a were the most active against Plasmodium falciparum strains. Structure-activity relationships demonstrated the importance of an enone moiety linked to the quinoxaline ring.
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ژورنال
عنوان ژورنال: European Journal of Medicinal Chemistry
سال: 2018
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2018.08.058