Aminopyridinecarboxamide-based inhibitors: Structure–activity relationship

Aminopyridinecarboxamide-based iKK-2 inhibitors were synthesized and tested leading to the 2-amino-5-chloropyridine-4-carboxamides as potent inhibitors with improved cellular activity. Series of aminopyridinecarboxamide-based inhibitors were synthesized and tested against human recombinant IKK-2 and...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry Vol. 18; no. 1; pp. 403 - 414
Main Authors:	Bonafoux, Dominique F., Bonar, Sheri L., Clare, Michael, Donnelly, Ann M., Glaenzer, Jeanette L., Guzova, Julia A., Huang, He, Kishore, Nandidni N., Koszyk, Francis J., Lennon, Patrick J., Libby, Adam, Mathialagan, Sumathy, Oburn, David S., Rouw, Sharon A, Sommers, Cynthia D., Tripp, Catherine S., Vanella, Lori J., Weier, Richard, Wolfson, Serge G., Huang, Horng-Chih
Format:	Journal Article
Language:	English
Published:	Amsterdam Elsevier Ltd 2010 Elsevier
Subjects:	Amides - chemistry Amides - pharmacology Amino Acid Sequence Aminopyrine - chemistry Aminopyrine - pharmacology Anti-Inflammatory Agents - chemistry Anti-Inflammatory Agents - pharmacology Arthritis, Rheumatoid - drug therapy Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Fibroblasts - drug effects Fibroblasts - immunology Humans I-kappa B Kinase - antagonists & inhibitors I-kappa B Kinase - metabolism I-kappa B Proteins - chemistry IKK2 Inhibitor Interleukin-1beta - antagonists & inhibitors Interleukin-1beta - metabolism Joint Capsule - cytology Medical sciences Molecular Sequence Data NFkB Pharmacology. Drug treatments Structure-Activity Relationship Inhibitor IKK2 NFkB Nitrogen heterocycle Morpholine derivatives Pyridine derivatives Signal transduction Structure activity relation Chlorine Organic compounds Six membered ring Aromatic compound Transcription factor NFκB Inhibition Chemical synthesis Interleukin 8 Enzyme Transferases Antiinflammatory agent Benzene derivatives Enzyme inhibitor Tricyclic compound In vitro Diamine Carboxamide Fluorine Organic compounds Piperazine derivatives Fibroblast
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Summary:	Aminopyridinecarboxamide-based iKK-2 inhibitors were synthesized and tested leading to the 2-amino-5-chloropyridine-4-carboxamides as potent inhibitors with improved cellular activity. Series of aminopyridinecarboxamide-based inhibitors were synthesized and tested against human recombinant IKK-2 and in IL-1β stimulated synovial fibroblasts. The 2-amino-5-chloropyridine-4-carboxamides were identified as the most potent inhibitors with improved cellular activity.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2009.10.040