دورية أكاديمية
Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.
| العنوان: | Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists. |
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| المؤلفون: | Shi Q; Eli Lilly and Company, Lilly Research Labs, Lilly Corporate Center, Indianapolis, IN 46285, USA. shi_qing@lilly.com, Canada EJ, Xu Y, Warshawsky AM, Etgen GJ, Broderick CL, Clutinger CK, Irwin LA, Laurila ME, Montrose-Rafizadeh C, Oldham BA, Wang M, Winneroski LL, Xie C, York JS, Yumibe NP, Zink RW, Mantlo N |
| المصدر: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Dec 15; Vol. 17 (24), pp. 6744-9. Date of Electronic Publication: 2007 Oct 18. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Ltd Original Publication: Oxford ; New York : Pergamon Press, c1991- |
| مواضيع طبية MeSH: | Drug Design*, Amides/*chemistry , Indoles/*chemical synthesis , PPAR delta/*agonists , PPAR gamma/*agonists, Animals ; Combinatorial Chemistry Techniques ; Diabetes Mellitus, Type 2/drug therapy ; Disease Models, Animal ; Indoles/chemistry ; Indoles/pharmacology ; Molecular Structure ; Rats |
| مستخلص: | A series of potent amide linked PPARgamma/delta dual agonists (1a) has been discovered through rational design. In the ZDF rat model of type 2 diabetes, compound (R)-3-[4-(3-{1-[(5-chloro-1,3-dimethyl-1H-indole-2-carbonyl)-amino]-ethyl}-5-fluoro-phenoxy)-2-ethyl-phenyl]-propionic acid (42) from this series has demonstrated glucose lowering efficacy comparable to the marketed PPARgamma agonist rosiglitazone with less weight gain. |
| المشرفين على المادة: | 0 ((R)-3-(4-(3-(1-((5-chloro-1,3-dimethyl-1H-indole-2-carbonyl)amino)ethyl)-5-fluoro-phenoxy)-2-ethylphenyl)propionic acid) 0 (Amides) 0 (Indoles) 0 (PPAR delta) 0 (PPAR gamma) |
| تواريخ الأحداث: | Date Created: 20071122 Date Completed: 20080303 Latest Revision: 20080213 |
| رمز التحديث: | 20221213 |
| DOI: | 10.1016/j.bmcl.2007.10.047 |
| PMID: | 18029178 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1464-3405 |
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| DOI: | 10.1016/j.bmcl.2007.10.047 |