Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4)
Autor(a) principal: | |
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Data de Publicação: | 2019 |
Outros Autores: | , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10316/101617 https://doi.org/10.1016/j.arabjc.2015.08.009 |
Resumo: | A series of novel hybrid molecules were designed rationally by connecting an indole moiety with a quinoxaline ring through a linker as potential inhibitors of PDE4. Their design was validated initially in silico by performing docking studies using a representative molecule. Subsequent synthesis of a focused library of related hybrid molecules was accomplished using Pd/CACu mediated coupling-cyclization as a key step. Some of the synthesized compounds showed PDE4 inhibition in vitro and one of them appeared to be promising. |
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7160 |
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Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4)IndoleQuinoxalinePd/CPDE4A series of novel hybrid molecules were designed rationally by connecting an indole moiety with a quinoxaline ring through a linker as potential inhibitors of PDE4. Their design was validated initially in silico by performing docking studies using a representative molecule. Subsequent synthesis of a focused library of related hybrid molecules was accomplished using Pd/CACu mediated coupling-cyclization as a key step. Some of the synthesized compounds showed PDE4 inhibition in vitro and one of them appeared to be promising.2019info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10316/101617http://hdl.handle.net/10316/101617https://doi.org/10.1016/j.arabjc.2015.08.009eng18785352Luther, Bethala JawaharRani, Chekuri SharmilaSuresh, NamburiBasaveswara Rao, Mandava V.Kapavarapu, RavikumarSuresh, ChakaliVijaya Babu, P.Pal, Manojitinfo:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2022-09-02T20:48:30Zoai:estudogeral.uc.pt:10316/101617Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T21:18:46.354302Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse |
dc.title.none.fl_str_mv |
Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4) |
title |
Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4) |
spellingShingle |
Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4) Luther, Bethala Jawahar Indole Quinoxaline Pd/C PDE4 |
title_short |
Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4) |
title_full |
Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4) |
title_fullStr |
Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4) |
title_full_unstemmed |
Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4) |
title_sort |
Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4) |
author |
Luther, Bethala Jawahar |
author_facet |
Luther, Bethala Jawahar Rani, Chekuri Sharmila Suresh, Namburi Basaveswara Rao, Mandava V. Kapavarapu, Ravikumar Suresh, Chakali Vijaya Babu, P. Pal, Manojit |
author_role |
author |
author2 |
Rani, Chekuri Sharmila Suresh, Namburi Basaveswara Rao, Mandava V. Kapavarapu, Ravikumar Suresh, Chakali Vijaya Babu, P. Pal, Manojit |
author2_role |
author author author author author author author |
dc.contributor.author.fl_str_mv |
Luther, Bethala Jawahar Rani, Chekuri Sharmila Suresh, Namburi Basaveswara Rao, Mandava V. Kapavarapu, Ravikumar Suresh, Chakali Vijaya Babu, P. Pal, Manojit |
dc.subject.por.fl_str_mv |
Indole Quinoxaline Pd/C PDE4 |
topic |
Indole Quinoxaline Pd/C PDE4 |
description |
A series of novel hybrid molecules were designed rationally by connecting an indole moiety with a quinoxaline ring through a linker as potential inhibitors of PDE4. Their design was validated initially in silico by performing docking studies using a representative molecule. Subsequent synthesis of a focused library of related hybrid molecules was accomplished using Pd/CACu mediated coupling-cyclization as a key step. Some of the synthesized compounds showed PDE4 inhibition in vitro and one of them appeared to be promising. |
publishDate |
2019 |
dc.date.none.fl_str_mv |
2019 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://hdl.handle.net/10316/101617 http://hdl.handle.net/10316/101617 https://doi.org/10.1016/j.arabjc.2015.08.009 |
url |
http://hdl.handle.net/10316/101617 https://doi.org/10.1016/j.arabjc.2015.08.009 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
18785352 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.source.none.fl_str_mv |
reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
instname_str |
Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
instacron_str |
RCAAP |
institution |
RCAAP |
reponame_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
collection |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
repository.name.fl_str_mv |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
repository.mail.fl_str_mv |
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1799134082272067584 |