The discovery of quinoline based single-ligand human H<sub>1</sub> and H<sub>3</sub> receptor antagonists.

Procopiou, Panayiotis A; Ancliff, Rachael A; Gore, Paul M; Hancock, Ashley P; Hodgson, Simon T; Holmes, Duncan S; Keeling, Steven P; Looker, Brian E; Parr, Nigel A; Rowedder, James E; Slack, Robert J

The discovery of quinoline based single-ligand human H₁ and H₃ receptor antagonists.

Procopiou, Panayiotis A; Ancliff, Rachael A; Gore, Paul M; Hancock, Ashley P; Hodgson, Simon T; Holmes, Duncan S; Keeling, Steven P; Looker, Brian E; Parr, Nigel A; Rowedder, James E; Slack, Robert J.

Afiliação

Procopiou PA; Medicinal Chemistry, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom. Electronic address: pan.a.procopiou@gsk.com.
Ancliff RA; Medicinal Chemistry, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.
Gore PM; Medicinal Chemistry, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.
Hancock AP; Medicinal Chemistry, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.
Hodgson ST; Medicinal Chemistry, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.
Holmes DS; Medicinal Chemistry, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.
Keeling SP; Medicinal Chemistry, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.
Looker BE; Medicinal Chemistry, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.
Parr NA; Medicinal Chemistry, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.
Rowedder JE; R&D Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.
Slack RJ; Respiratory Biology, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.

Bioorg Med Chem Lett ; 26(24): 5855-5859, 2016 12 15.

Article em En | MEDLINE | ID: mdl-27866818

Assuntos

Descoberta de Drogas; Antagonistas dos Receptores Histamínicos H1/farmacologia; Antagonistas dos Receptores Histamínicos H3/farmacologia; Quinolinas/farmacologia; Receptores Histamínicos H1/metabolismo; Receptores Histamínicos H3/metabolismo; Relação Dose-Resposta a Droga; Antagonistas dos Receptores Histamínicos H1/síntese química; Antagonistas dos Receptores Histamínicos H1/química; Antagonistas dos Receptores Histamínicos H3/síntese química; Antagonistas dos Receptores Histamínicos H3/química; Humanos; Ligantes; Estrutura Molecular; Quinolinas/síntese química; Quinolinas/química; Relação Estrutura-Atividade

Palavras-chave

Allergic rhinitis; H(1)H(3) histamine receptor antagonist; Nasal congestion; Quinoline; Single ligand

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Quinolinas / Receptores Histamínicos H1 / Receptores Histamínicos H3 / Antagonistas dos Receptores Histamínicos H3 / Descoberta de Drogas / Antagonistas dos Receptores Histamínicos H1 Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2016 Tipo de documento: Article

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