Synthesis and evaluation of 4,5-dihydro-5-methylisoxazolin-5-carboxamide derivatives as VLA-4 antagonists.

Soni, Ajay; Rehman, Abdul; Naik, Keshav; Dastidar, Sunanda; Alam, M S; Ray, Abhijit; Chaira, Tridib; Shah, Vanya; Palle, Venkata P; Cliffe, Ian A; Sattigeri, Viswajanani J

Soni, Ajay; Rehman, Abdul; Naik, Keshav; Dastidar, Sunanda; Alam, M S; Ray, Abhijit; Chaira, Tridib; Shah, Vanya; Palle, Venkata P; Cliffe, Ian A; Sattigeri, Viswajanani J.

Afiliação

Soni A; Department of Medicinal Chemistry, New Drug Discovery Research, Ranbaxy Research Laboratories, Plot 20, Sector 18, Gurgaon 122015, Haryana, India. ajay_soni_78@yahoo.com

Bioorg Med Chem Lett ; 23(5): 1482-5, 2013 Mar 01.

Article em En | MEDLINE | ID: mdl-23312947

ABSTRACT

ABSTRACT

A novel set of compounds containing a 4,5-dihydro-5-methylisoxazoline have been successfully designed as VLA-4 receptor antagonists. Compound (14p) had a high receptor binding affinity of 4 nM and also found to be metabolically stable in vitro.

Assuntos

Integrina alfa4beta1/antagonistas & inibidores; Isoxazóis/química; Isoxazóis/farmacologia; Amidas/síntese química; Amidas/química; Amidas/farmacologia; Estabilidade de Medicamentos; Humanos; Integrina alfa4beta1/química; Isoxazóis/síntese química; Ligação Proteica; Relação Estrutura-Atividade; Células U937

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Integrina alfa4beta1 / Isoxazóis Limite: Humans Idioma: En Ano de publicação: 2013 Tipo de documento: Article

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