Synthesis and biological activity of N-substituted aminocarbonyl-1,3-dioxolanes as VLA-4 antagonists. 2010

Abdul Rehman, and Ajay Soni, and Keshav Naik, and Sreeji Nair, and Venkata P Palle, and Sunanda Dastidar, and Abhijit Ray, and M S Alam, and Mohammad Salman, and Ian A Cliffe, and Viswajanani Sattigeri
Department of Medicinal Chemistry, New Drug Discovery Research, Ranbaxy Research Laboratories, Plot 20, Sector 18, Gurgaon 122015, Haryana, India. ab_rehman@rediffmail.com

A novel set of compounds with a 1,3-dioxolane ring which acts as a proline bioisostere have been successfully designed as VLA-4 receptor antagonists. Compounds (18e), (28j), and (35g) were shown to have high receptor affinities.

UI MeSH Term Description Entries
D008958 Models, Molecular Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures. Molecular Models,Model, Molecular,Molecular Model
D011485 Protein Binding The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments. Plasma Protein Binding Capacity,Binding, Protein
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D004148 Dioxolanes
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
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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