About: Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus

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About: Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus
Creator	Gazzarrini, Sabrina Moroni, Anna Naesens, Lieve Cichero, Elena Loddo, Roberta »more»
source	Elsevier; Medline; PMC
abstract	Abstract We have identified a series of 1-aryl-4,6-diamino-1,2-dihydrotriazines, structurally related to the antimalarial drug cycloguanil, as new inhibitors of influenza A and B virus and respiratory syncytial virus (RSV) via targeting of the host dihydrofolate reductase (DHFR) enzyme. Most analogues proved active against influenza B virus in the low micromolar range, and the best compounds (11, 13, 14 and 16) even reached the sub-micromolar potency of zanamivir (EC50 = 0.060 μM), and markedly exceeded (up to 327 times) the antiviral efficacy of ribavirin. Activity was also observed for two influenza A strains, including a virus with the S31N mutant form of M2 proton channel, which is the most prevalent resistance mutation for amantadine. Importantly, the compounds displayed nanomolar activity against RSV and a superior selectivity index, since the ratio of cytotoxic to antiviral concentration was >10,000 for the three most active compounds 11, 14 and 16 (EC50 ∼0.008 μM), far surpassing the potency and safety profile of the licensed drug ribavirin (EC50 = 5.8 μM, SI > 43).
has issue date	2017-07-28(xsd:dateTime)
bibo:doi	10.1016/j.ejmech.2017.04.070
bibo:pmid	28477572
has license	els-covid
sha1sum (hex)	779c7d7dd2bd01cee9a84467009ed38b59466135
schema:url	https://doi.org/10.1016/j.ejmech.2017.04.070
resource representing a document's title	Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus
has PubMed Central identifier	PMC7115580
has PubMed identifier	28477572
schema:publication	European Journal of Medicinal Chemistry
resource representing a document's body	covid:779c7d7dd2bd01cee9a84467009ed38b59466135#body_text
is schema:about of	covid:arg/779c7d7dd2bd01cee9a84467009ed38b59466135 named entity 'activity' named entity 'DHFR' named entity 'dihydrofolate reductase' named entity 'protozoal' »more»

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