دورية أكاديمية
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
| العنوان: | Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators. |
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| المؤلفون: | Martinborough E; Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center Drive, San Diego, California 92121, USA., Shen Y, Oeveren Av, Long YO, Lau TL, Marschke KB, Chang WY, López FJ, Vajda EG, Rix PJ, Viveros OH, Negro-Vilar A, Zhi L |
| المصدر: | Journal of medicinal chemistry [J Med Chem] 2007 Oct 18; Vol. 50 (21), pp. 5049-52. Date of Electronic Publication: 2007 Sep 21. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Print ISSN: 0022-2623 (Print) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Washington Dc : American Chemical Society Original Publication: [Easton, Pa.] : American Chemical Society, [c1963- |
| مواضيع طبية MeSH: | Androgen Receptor Antagonists* , Androgens*, Anabolic Agents/*chemical synthesis , Bone Density Conservation Agents/*chemical synthesis , Pyrrolidines/*chemical synthesis , Quinolines/*chemical synthesis , Quinolones/*chemical synthesis, Administration, Oral ; Anabolic Agents/pharmacokinetics ; Anabolic Agents/pharmacology ; Animals ; Biological Availability ; Bone Density Conservation Agents/pharmacokinetics ; Bone Density Conservation Agents/pharmacology ; Female ; Humans ; Hypogonadism/drug therapy ; Hypogonadism/pathology ; Male ; Muscle, Skeletal/drug effects ; Muscle, Skeletal/metabolism ; Organ Size/drug effects ; Osteoporosis, Postmenopausal/drug therapy ; Prostate/drug effects ; Pyrrolidines/pharmacokinetics ; Pyrrolidines/pharmacology ; Quinolines/pharmacokinetics ; Quinolines/pharmacology ; Quinolones/pharmacokinetics ; Quinolones/pharmacology ; Rats ; Stereoisomerism ; Structure-Activity Relationship |
| مستخلص: | The androgen receptor is a ligand inducible transcription factor that is involved in a broad range of physiological functions. Here we describe the discovery of a new class of orally available selective androgen receptor modulators. The lead compound, 6-[(2R,5R)-2-methyl-5-((R)-2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl]-4-trifluoromethylquinolin-2(1H)-one (6a), showed excellent anabolic activity in muscle with reduced effect on the prostate in a rat model of hypogonadism. The compound also improved bone strength in a rat model of post-menopausal osteoporosis. |
| المشرفين على المادة: | 0 (6-(2-methyl-5-(2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl)-4-trifluoromethylquinolin-2(1H)-one) 0 (Anabolic Agents) 0 (Androgen Receptor Antagonists) 0 (Androgens) 0 (Bone Density Conservation Agents) 0 (Pyrrolidines) 0 (Quinolines) 0 (Quinolones) |
| تواريخ الأحداث: | Date Created: 20070925 Date Completed: 20071127 Latest Revision: 20101118 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1021/jm070231h |
| PMID: | 17887661 |
| قاعدة البيانات: | MEDLINE |
Find this issue from the American Chemical Society | تدمد: | 0022-2623 |
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| DOI: | 10.1021/jm070231h |