Antagonists of the adenosine A<sub>2A</sub> receptor based on a 2-arylbenzoxazole scaffold: Investigation of the C5- and C7-positions to enhance affinity.

Duroux, Romain; Agouridas, Laurence; Renault, Nicolas; El Bakali, Jamal; Furman, Christophe; Melnyk, Patricia; Yous, Saïd

Antagonists of the adenosine A_2A receptor based on a 2-arylbenzoxazole scaffold: Investigation of the C5- and C7-positions to enhance affinity.

Duroux, Romain; Agouridas, Laurence; Renault, Nicolas; El Bakali, Jamal; Furman, Christophe; Melnyk, Patricia; Yous, Saïd.

Afiliação

Duroux R; Univ. Lille, Inserm, CHU Lille, UMR-S1172 - JPArc - Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer, F-59000 Lille, France.
Agouridas L; Univ. Lille, Inserm, CHU Lille, UMR-S1172 - JPArc - Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer, F-59000 Lille, France.
Renault N; Univ. Lille, Inserm, CHU Lille, U995 - LIRIC - Lille Inflammation Research International Center, F-59000 Lille, France.
El Bakali J; Univ. Lille, Inserm, CHU Lille, UMR-S1172 - JPArc - Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer, F-59000 Lille, France.
Furman C; Univ. Lille, Inserm, CHU Lille, U995 - LIRIC - Lille Inflammation Research International Center, F-59000 Lille, France.
Melnyk P; Univ. Lille, Inserm, CHU Lille, UMR-S1172 - JPArc - Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer, F-59000 Lille, France.
Yous S; Univ. Lille, Inserm, CHU Lille, UMR-S1172 - JPArc - Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer, F-59000 Lille, France. Electronic address: said.yous@univ-lille2.fr.

Eur J Med Chem ; 144: 151-163, 2018 Jan 20.

Article em En | MEDLINE | ID: mdl-29268131

Assuntos

Antagonistas do Receptor A2 de Adenosina/química; Antagonistas do Receptor A2 de Adenosina/farmacologia; Benzoxazóis/química; Benzoxazóis/farmacologia; Receptor A2A de Adenosina/metabolismo; Antagonistas do Receptor A2 de Adenosina/metabolismo; Antagonistas do Receptor A2 de Adenosina/farmacocinética; Benzoxazóis/metabolismo; Benzoxazóis/farmacocinética; Células CACO-2; Linhagem Celular Tumoral; Desenho de Fármacos; Humanos; Microssomos Hepáticos/metabolismo; Solubilidade

Palavras-chave

A(2A) receptor; Benzoxazole; DMPK; Neurodegenerative disease

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Benzoxazóis / Receptor A2A de Adenosina / Antagonistas do Receptor A2 de Adenosina Idioma: En Ano de publicação: 2018 Tipo de documento: Article

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