Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: Structural requirements for better physicochemical and biological properties
| Autor: | Motonori Miyakawa, Noriko Yamamoto, Naoya Nagata, Kazuyuki Furuya, Kiyoshi Inoguchi, Seiji Amano, Hiroaki Nejishima |
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| Rok vydání: | 2011 |
| Předmět: |
Femoral bone mineral density
Nonsteroidal Chemistry Ovariectomy Organic Chemistry Clinical Biochemistry Pharmaceutical Science Pharmacology Biochemistry In vitro Rats Androgen receptor chemistry.chemical_compound Bone Density Receptors Androgen Biological property Drug Discovery Quinolines Ovariectomized rat Animals Osteoporosis Molecular Medicine Female Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 21:6310-6313 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2011.08.118 |
| Popis: | A rationally designed tetrahydroquinoline (1) for nonsteroidal selective androgen receptor modulators was modified for the exploration of promising compounds by Grieco three-component condensation using various dienophiles. Based on the in vitro effects and physicochemical properties of the synthesized compounds, compound 4c was selected for further study. Compound 4c increased the femoral bone mineral density as much as DHT, but it reduced the uterus effect compared with DHT in ovariectomized rats. Thus, compound 4c has desirable osteoanabolic effects with weak undesirable effects on the uterus in a female osteoporosis model. |
| Databáze: | OpenAIRE |
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