Discovery of Potent Dual PPARα Agonists/CB1 Ligands
| العنوان: | Discovery of Potent Dual PPARα Agonists/CB1 Ligands |
|---|---|
| المؤلفون: | Ruth Pérez-Fernández, Fernando Rodríguez de Fonseca, Juan Decara, Pilar Goya, Rocío Girón, Nieves Fresno, Ana Rodríguez-Álvarez, José Elguero, María Isabel Martín, Manuel Macias-Gonzalez |
| المصدر: | ACS Medicinal Chemistry Letters; Vol 2 Digital.CSIC. Repositorio Institucional del CSIC instname ACS Medicinal Chemistry Letters |
| سنة النشر: | 2011 |
| مصطلحات موضوعية: | Cannabinoid receptor, medicine.medical_treatment, Peroxisome proliferator-activated receptor, cannabinoids, Biochemistry, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Rimonabant, Drug Discovery, medicine, Receptor, 030304 developmental biology, chemistry.chemical_classification, 0303 health sciences, Organic Chemistry, neuroprotective, Combinatorial chemistry, 3. Good health, Dual ligands, chemistry, rimonabant, 030220 oncology & carcinogenesis, Cannabinoid receptor antagonist, lipids (amino acids, peptides, and proteins), Cannabinoid, fibrates, Pharmacophore, Lead compound, PPARα, medicine.drug |
| الوصف: | ABSTRACT: This letter describes the synthesis and in vitro and in vivo evaluation of dual ligands targeting the cannabinoid and peroxisome proliferator-activated receptors (PPAR). These com- pounds were obtained from fusing the pharmacophores of fibrates and the diarylpyrazole rimonabant, a cannabinoid receptor an- tagonist. They are the first examples of dual compounds with nanomolar affinity for both PPARα and cannabinoid receptors. Besides, lead compound 2 proved to be CB1 selective. Unexpect- edly, the phenol intermediates tested were equipotent (compound 1 as compared to 2) or even more potent (compound 3 as compared with 4). This discovery opens the way to design new dual ligands. |
| تدمد: | 1948-5875 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::30c95c893720bb7321f67d6572fb0d04Test https://pubmed.ncbi.nlm.nih.gov/24936232Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....30c95c893720bb7321f67d6572fb0d04 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 19485875 |
|---|