- Epiminocyclohepta[b]indole analogs as 5-HT6 antagonists
[作者:Henderson, AJ; Guzzo, PR; Ghosh, A; Kaur, J; Koo, JM; Nacro, K; Panduga, S; Pathak, R; Shimpukade, B; Tan, V; Xiang, K; Wierschke, JD; Isherwood, ML,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1494-1498 , 文章类型: Article,,卷期:2012年22-4]
- A new series of epiminocyclohepta[b]indoles with potent 5-HT6 antagonist activity were discovered and optimized using in vitro protocols. One compound from this series was progressed to advanced pharmacokinetic (PK) stud...
- 4-Phenoxypiperidine pyridazin-3-one histamine H-3 receptor inverse agonists demonstrating potent and robust wake promoting activity
[作者:Hudkins, RL; Zulli, AL; Dandu, RR; Tao, M; Josef, KA; Aimone, LD; Haltiwanger, RC; Huang, ZQ; Lyons, JA; Mathiasen, JR; Raddatz, R; Gruner, JA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1504-1509 , 文章类型: Article,,卷期:2012年22-4]
- Structure-activity relationships for a series of phenoxypiperidine pyridazin-3-one H3R antagonists/inverse agonists are disclosed. The search for compounds with improved hERG and DAT selectivity without the formation of ...
- Inhibitors of acetyltransferase domain of N-acetylglucosamine-1-phosphate-uridyltransferase/glucosamine-1-phosphate-acetyltransferase (GlmU). Part 1: Hit to lead evaluation of a novel arylsulfonamide series
[作者:Green, OM; McKenzie, AR; Shapiro, AB; Otterbein, L; Ni, HH; Patten, A; Stokes, S; Albert, R; Kawatkar, S; Breed, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1510-1519 , 文章类型: Article,,卷期:2012年22-4]
- A novel arylsulfonamide-containing series of compounds represented by 1, discovered by highthrough-put screening, inhibit the acetyltransferase domain of N-acetylglucosamine-1-phosphate-uridyltransferase/glucosamine-1-ph...
- Dual beta(2)-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD
[作者:Shan, WJ; Huang, L; Zhou, Q; Jiang, HL; Luo, ZH; Lai, KF; Li, XS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1523-1526 , 文章类型: Article,,卷期:2012年22-4]
- We designed and synthesized a novel class of dual pharmacology bronchodilators targeting both beta 2-adrenoceptor and PDE4 by applying a multivalent approach. The most potent dual pharmacology molecule, compound 29, poss...
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