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dc.contributor.author
Bollini, Mariela  
dc.contributor.author
Cisneros, José A.  
dc.contributor.author
Spasov, Krasimir A.  
dc.contributor.author
Anderson, Karen S.  
dc.contributor.author
Jorgensen, William L.  
dc.date.available
2017-09-21T21:16:33Z  
dc.date.issued
2013-07  
dc.identifier.citation
Bollini, Mariela; Cisneros, José A.; Spasov, Krasimir A.; Anderson, Karen S.; Jorgensen, William L.; Optimization of diarylazines as anti-HIV agents with dramatically; Elsevier; Bioorganic & Medicinal Chemistry Letters; 23; 18; 7-2013; 5213-5216  
dc.identifier.issn
0960-894X  
dc.identifier.uri
http://hdl.handle.net/11336/24881  
dc.description.abstract
Non-nucleoside inhibitors of HIV-1 reverse transcriptase are reported that have ca. 100-fold greater solubility than the structurally related drugs etravirine and rilpivirine, while retaining high anti-viral activity. The solubility enhancements come from strategic placement of a morpholinylalkoxy substituent in the entrance channel of the NNRTI binding site. Compound 4d shows low-nanomolar activity similar to etravirine towards wild-type HIV-1 and key viral variants.  
dc.format
application/pdf  
dc.language.iso
eng  
dc.publisher
Elsevier  
dc.rights
info:eu-repo/semantics/openAccess  
dc.rights.uri
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/  
dc.subject
Anti-Hiv Agent  
dc.subject
Nnrti  
dc.subject
Drug Solubility  
dc.subject.classification
Otras Ciencias Químicas  
dc.subject.classification
Ciencias Químicas  
dc.subject.classification
CIENCIAS NATURALES Y EXACTAS  
dc.title
Optimization of diarylazines as anti-HIV agents with dramatically  
dc.type
info:eu-repo/semantics/article  
dc.type
info:ar-repo/semantics/artículo  
dc.type
info:eu-repo/semantics/publishedVersion  
dc.date.updated
2017-09-21T18:55:45Z  
dc.journal.volume
23  
dc.journal.number
18  
dc.journal.pagination
5213-5216  
dc.journal.pais
Países Bajos  
dc.journal.ciudad
Ámsterdam  
dc.description.fil
Fil: Bollini, Mariela. University of Yale; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina  
dc.description.fil
Fil: Cisneros, José A.. University of Yale; Estados Unidos  
dc.description.fil
Fil: Spasov, Krasimir A.. University of Yale; Estados Unidos  
dc.description.fil
Fil: Anderson, Karen S.. University of Yale; Estados Unidos  
dc.description.fil
Fil: Jorgensen, William L.. University of Yale; Estados Unidos  
dc.journal.title
Bioorganic & Medicinal Chemistry Letters  
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.bmcl.2013.06.091  
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0960894X1300824X  
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3759246/  

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