Optimization of diarylazines as anti-HIV agents with dramatically

Autores
Bollini, Mariela; Cisneros, José A.; Spasov, Krasimir A.; Anderson, Karen S.; Jorgensen, William L.
Año de publicación
2013
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
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.
Fil: Bollini, Mariela. University of Yale; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Cisneros, José A.. University of Yale; Estados Unidos
Fil: Spasov, Krasimir A.. University of Yale; Estados Unidos
Fil: Anderson, Karen S.. University of Yale; Estados Unidos
Fil: Jorgensen, William L.. University of Yale; Estados Unidos
Materia
Anti-HIV agent
NNRTI
Drug solubility
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/24881
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/24881
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Optimization of diarylazines as anti-HIV agents with dramaticallyBollini, MarielaCisneros, José A.Spasov, Krasimir A.Anderson, Karen S.Jorgensen, William L.Anti-HIV agentNNRTIDrug solubilityhttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1Non-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.Fil: Bollini, Mariela. University of Yale; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Cisneros, José A.. University of Yale; Estados UnidosFil: Spasov, Krasimir A.. University of Yale; Estados UnidosFil: Anderson, Karen S.. University of Yale; Estados UnidosFil: Jorgensen, William L.. University of Yale; Estados UnidosElsevier2013-07info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/24881Bollini, 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; 5213-52160960-894XCONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.1016/j.bmcl.2013.06.091info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0960894X1300824Xinfo:eu-repo/semantics/altIdentifier/url/https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3759246/info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-nd/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-11-12T09:48:06Zoai:ri.conicet.gov.ar:11336/24881instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-11-12 09:48:06.622CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Optimization of diarylazines as anti-HIV agents with dramatically
title Optimization of diarylazines as anti-HIV agents with dramatically
spellingShingle Optimization of diarylazines as anti-HIV agents with dramatically
Bollini, Mariela
Anti-HIV agent
NNRTI
Drug solubility
title_short Optimization of diarylazines as anti-HIV agents with dramatically
title_full Optimization of diarylazines as anti-HIV agents with dramatically
title_fullStr Optimization of diarylazines as anti-HIV agents with dramatically
title_full_unstemmed Optimization of diarylazines as anti-HIV agents with dramatically
title_sort Optimization of diarylazines as anti-HIV agents with dramatically
dc.creator.none.fl_str_mv Bollini, Mariela
Cisneros, José A.
Spasov, Krasimir A.
Anderson, Karen S.
Jorgensen, William L.
author Bollini, Mariela
author_facet Bollini, Mariela
Cisneros, José A.
Spasov, Krasimir A.
Anderson, Karen S.
Jorgensen, William L.
author_role author
author2 Cisneros, José A.
Spasov, Krasimir A.
Anderson, Karen S.
Jorgensen, William L.
author2_role author
author
author
author
dc.subject.none.fl_str_mv Anti-HIV agent
NNRTI
Drug solubility
topic Anti-HIV agent
NNRTI
Drug solubility
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv 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.
Fil: Bollini, Mariela. University of Yale; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Cisneros, José A.. University of Yale; Estados Unidos
Fil: Spasov, Krasimir A.. University of Yale; Estados Unidos
Fil: Anderson, Karen S.. University of Yale; Estados Unidos
Fil: Jorgensen, William L.. University of Yale; Estados Unidos
description 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.
publishDate 2013
dc.date.none.fl_str_mv 2013-07
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/24881
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
0960-894X
CONICET Digital
CONICET
url http://hdl.handle.net/11336/24881
identifier_str_mv 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
0960-894X
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1016/j.bmcl.2013.06.091
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0960894X1300824X
info:eu-repo/semantics/altIdentifier/url/https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3759246/
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
_version_ 1848597987588046848
score 13.25334

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