Abstract
Modification on a lead series of [1,4]oxazino[3,2-g]quinolin-7-ones at the 2-position led to selective androgen receptor modulators with improved in vivo activity. The most potent analog (-)-33a exhibited full maintenance of levator ani muscle at 3mg/kg and reduced activity on ventral prostate weight in a 2-week orally-dosed and orchidectomized rat maintenance assay.
MeSH terms
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Administration, Oral
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Anabolic Agents / chemical synthesis
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Anabolic Agents / pharmacology*
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Androgen Receptor Antagonists
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Androgens
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Animals
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Male
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Models, Chemical
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Orchiectomy
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Organ Size / drug effects
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Oxazines / chemical synthesis
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Oxazines / pharmacology*
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Prostate / anatomy & histology
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Prostate / drug effects*
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Quinolones / chemical synthesis
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Quinolones / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Receptors, Androgen*
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Structure-Activity Relationship
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Testosterone / pharmacology
Substances
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Anabolic Agents
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Androgen Receptor Antagonists
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Androgens
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Oxazines
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Quinolones
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Receptors, Androgen
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Testosterone