Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists

التفاصيل البيبلوغرافية
العنوان: Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists
المؤلفون: Daniel R. Mudra, Matthew J. Fisher, Maria-Jesus Blanco, Warshawsky Alan M, Xiao-Peng Yu, Tatiana Natali Vetman, Anita K. Harvey, Srinivasan Chandrasekhar, Xushan Wang, Kuklish Steven Lee, J.L. Oskins, Mark Chambers, C. Lin
المصدر: Bioorganic & Medicinal Chemistry Letters. 26:2303-2307
بيانات النشر: Elsevier BV, 2016.
سنة النشر: 2016
مصطلحات موضوعية: 0301 basic medicine, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Benzoates, Biochemistry, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Diclofenac, X-Ray Diffraction, In vivo, Drug Discovery, Pyridine, medicine, Animals, Molecular Biology, IC50, Benzoic acid, Whole blood, Organic Chemistry, Biological activity, Rats, 030104 developmental biology, chemistry, 030220 oncology & carcinogenesis, Molecular Medicine, Receptors, Prostaglandin E, EP4 Subtype, Ex vivo, medicine.drug
الوصف: Continued SAR optimization of a series of 3-methylpyridine-2-carbonyl amino-2,4-dimethyl-benzoic acid led to the selection of compound 4f for clinical studies. Compound 4f showed an IC50 of 123nM for inhibition of PGE2-induced TNFα reduction in an ex vivo LPS-stimulated human whole blood assay (showing >10-fold increase over clinical compound CJ-023,423). Pharmacokinetic profile, selectivity and in vivo efficacy comparing 4f to NSAID diclofenac in the monoiodoacetic acid (MIA) pain model and adjuvant induced arthritis (AIA) inflammatory model are included.
تدمد: 0960-894X
DOI: 10.1016/j.bmcl.2016.03.041
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::14c5fc831a41c4d4dae2d9bc322b91a3
https://doi.org/10.1016/j.bmcl.2016.03.041
Rights: CLOSED
رقم الانضمام: edsair.doi.dedup.....14c5fc831a41c4d4dae2d9bc322b91a3
قاعدة البيانات: OpenAIRE
الوصف
تدمد:0960894X
DOI:10.1016/j.bmcl.2016.03.041