2,6-Quinolinyl derivatives as potent VLA-4 antagonists. 2007

Marie-Agnès Lassoie, and Fabienne Broeders, and Philippe Collart, and Laurent Defrère, and Françoise de Laveleye-Defais, and Thierry Demaude, and Abdoulaye Gassama, and Gérald Guillaumet, and Jean-Claude Hayez, and Laszlo Kiss, and Laurent Knerr, and Jean-Marie Nicolas, and Stéphanie Norsikian, and Luc Quéré, and Sylvain Routier, and Valérie Verbois, and Laurent Provins
UCB S.A., R&D, Chemin du Foriest, B-1420 Braine-l'Alleud, Belgium.

A new series of 2,6-quinolinyl derivatives was prepared leading to potent low nanomolar VLA-4/VCAM-1 antagonists.

UI MeSH Term Description Entries
D011804 Quinolines
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000894 Anti-Inflammatory Agents, Non-Steroidal Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects. Analgesics, Anti-Inflammatory,Aspirin-Like Agent,Aspirin-Like Agents,NSAID,Non-Steroidal Anti-Inflammatory Agent,Non-Steroidal Anti-Inflammatory Agents,Nonsteroidal Anti-Inflammatory Agent,Anti Inflammatory Agents, Nonsteroidal,Antiinflammatory Agents, Non Steroidal,Antiinflammatory Agents, Nonsteroidal,NSAIDs,Nonsteroidal Anti-Inflammatory Agents,Agent, Aspirin-Like,Agent, Non-Steroidal Anti-Inflammatory,Agent, Nonsteroidal Anti-Inflammatory,Anti-Inflammatory Agent, Non-Steroidal,Anti-Inflammatory Agent, Nonsteroidal,Anti-Inflammatory Analgesics,Aspirin Like Agent,Aspirin Like Agents,Non Steroidal Anti Inflammatory Agent,Non Steroidal Anti Inflammatory Agents,Nonsteroidal Anti Inflammatory Agent,Nonsteroidal Anti Inflammatory Agents,Nonsteroidal Antiinflammatory Agents
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D039041 Integrin alpha4beta1 Integrin alpha4beta1 is a FIBRONECTIN and VCAM-1 receptor present on LYMPHOCYTES; MONOCYTES; EOSINOPHILS; NK CELLS and thymocytes. It is involved in both cell-cell and cell- EXTRACELLULAR MATRIX adhesion and plays a role in INFLAMMATION, hematopoietic cell homing and immune function, and has been implicated in skeletal MYOGENESIS; NEURAL CREST migration and proliferation, lymphocyte maturation and morphogenesis of the PLACENTA and HEART. CD49d-CD29,Integrin Heterodimer alpha4beta1,Integrin alpha(4)beta(1),VLA-4,Very Late Activation Antigen-4,Very Late Antigen-4,alpha4beta1 Integrin,Antigen-4, Very Late,Heterodimer alpha4beta1, Integrin,Integrin, alpha4beta1,Late Antigen-4, Very,Very Late Activation Antigen 4,Very Late Antigen 4,alpha4beta1, Integrin,alpha4beta1, Integrin Heterodimer

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