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dc.contributor.author
Bollini, Mariela  
dc.contributor.author
Frey, Kathleen M.  
dc.contributor.author
Cisneros, José A.  
dc.contributor.author
Spasov, Krasimir A.  
dc.contributor.author
Das, Kalyan  
dc.contributor.author
Bauman, Joseph D.  
dc.contributor.author
Arnold, Eddy  
dc.contributor.author
Anderson, Karen S.  
dc.contributor.author
Jorgensen, William L.  
dc.date.available
2017-05-17T20:28:50Z  
dc.date.issued
2013-08  
dc.identifier.citation
Bollini, Mariela; Frey, Kathleen M.; Cisneros, José A.; Spasov, Krasimir A.; Das, Kalyan; et al.; Extension into the entrance channel of HIV-1 reverse transcriptase—Crystallography and enhanced solubility; Elsevier; Bioorganic & Medicinal Chemistry Letters; 23; 18; 8-2013; 5209-5212  
dc.identifier.issn
0960-894X  
dc.identifier.uri
http://hdl.handle.net/11336/16594  
dc.description.abstract
Non-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-RT) are reported that feature extension into the entrance channel near Glu138. Complexes of the parent anilinylpyrimidine 1 and the morpholinoethoxy analog 2j with HIV-RT have received crystallographic characterization confirming the designs. Measurement of aqueous solubilities of 2j, 2k, the parent triazene 2a, and other NNRTIs demonstrate profound benefits for addition of the morpholinyl substituent.  
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
Crystal Structures  
dc.subject
Drug Solubility  
dc.subject.classification
Química Orgánica  
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Ciencias Químicas  
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CIENCIAS NATURALES Y EXACTAS  
dc.title
Extension into the entrance channel of HIV-1 reverse transcriptase—Crystallography and enhanced solubility  
dc.type
info:eu-repo/semantics/article  
dc.type
info:ar-repo/semantics/artículo  
dc.type
info:eu-repo/semantics/publishedVersion  
dc.date.updated
2017-05-15T14:45:24Z  
dc.journal.volume
23  
dc.journal.number
18  
dc.journal.pagination
5209-5212  
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: Frey, Kathleen M.. University of Yale. School of Medicine; Estados Unidos  
dc.description.fil
Fil: Cisneros, José A.. University of Yale; Estados Unidos  
dc.description.fil
Fil: Spasov, Krasimir A.. University of Yale. School of Medicine; Estados Unidos  
dc.description.fil
Fil: Das, Kalyan. Rutgers University; Estados Unidos  
dc.description.fil
Fil: Bauman, Joseph D.. Rutgers University; Estados Unidos  
dc.description.fil
Fil: Arnold, Eddy. Rutgers University; Estados Unidos  
dc.description.fil
Fil: Anderson, Karen S.. University of Yale. School of Medicine; 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.2013.06.093  
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0960894X13008263