- Synthesis and In Vitro Opioid Receptor Functional Antagonism of Methyl-Substituted Analogues of (3R)-7-Hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic)
[作者:CUEVA JUAN PABLO; CAI TINGWEI BILL; MASCARELLA S WAYNE; THOMAS JAMES B; NAVARRO HERNAN A; CARROLL F IVY,期刊:Journal of Medicinal Chemistry, 页码:7463-7472 , 文章类型: Article,,卷期:2009年52-23]
- In previous structure-activity relationship (SAR) studies, (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-p iperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinoline-ca rboxamide (JDTic,...
- (3R,5S,7as)-(3,5-Bis(4-fluorophenyl)tetrahydro-1H-oxazolo[3,4-c]oxazol-7a-yl)methanol, a Novel Neuroprotective Agent
[作者:DESINO KELLY E; ANSAR SABAH; GEORG GUNDA I; HIMES RICHARD H; MICHAELIS MARY LOU; POWELL DOUGLAS R; REIFF EMILY A; TELIKEPALLI HANUMAIAH; AUDUS KENNETH L,期刊:Journal of Medicinal Chemistry, 页码:7537-7543 , 文章类型: Article,,卷期:2009年52-23]
- Compounds that interact with microtubules, such as paclitaxel, have been shown to possess protective properties against beta-amyloid (A beta) induced neurodegeneration associated with Alzheimer's disease. In this work, t...
- A Strategy to Minimize Reactive Metabolite Formation: Discovery of (S)-4-(1-Cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a Potent, Orally Bioavailable Corticotropin-Releasing Factor-1 Receptor Antagonist
[作者:HARTZ RICHARD A; AHUJA VIJAY T; ZHUO XIAOLIANG; MATTSON RONALD J; DENHART DEREK J; DESKUS JEFFREY A; VRUDHULA VIVEKANANDA M; PAN SENLIANG; DITTA JONATHAN L; SHU YUEZHONG; GRACE JAMES E; LENTZ KIMBERLEY A; LELAS SNJEZANA; LI YUWEN; MOLSKI THADDEUS F; KRISHNANANTHAN SUBRAMANIAM; WONG HENRY; QIANCUTRONE JINGFANG; SCHARTMAN RICHARD; DENTON REX; LODGE NICHOLAS J; ZACZEK ROBERT; MACOR JOHN E; BRONSON JOANNE J,期刊:Journal of Medicinal Chemistry, 页码:7653-7668 , 文章类型: Article,,卷期:2009年52-23]
- Detailed metabolic characterization of 8, an earlier lead pyrazinone-based corticotropin-releasing factor-1 (CRF1) receptor antagonist, revealed that this compound formed significant levels of reactive metabolites, its m...
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