- Aleglitazar, a new, potent, and balanced dual PPAR alpha/gamma agonist for the treatment of type II diabetes
[作者:Benardeau, A; Benz, J; Binggeli, A; Blum, D; Boehringer, M; Grether, U; Hilpert, H; Kuhn, B; Marki, HP; Meyer, M; Puntener, K; Raab, S; Ruf, A; Schlatter, D; Mohr, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2468-2473 , 文章类型: Article,,卷期:2009年19-9]
- Design, synthesis, and SAR of novel alpha-alkoxy-beta-arylpropionic acids as potent and balanced PPAR alpha gamma coagonists are described. One representative thereof, Aleglitazar ((S)-2Aa), was chosen for clinical devel...
- Synthesis of conjugated spermine derivatives with 7-nitrobenzoxadiazole (NBD), rhodamine and bodipy as new fluorescent probes for the polyamine transport system
[作者:Guminski, Y; Grousseaud, M; Cugnasse, S; Brel, V; Annereau, JP; Vispe, S; Guilbaud, N; Barret, JM; Bailly, C; Imbert, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2474-2477 , 文章类型: Article,,卷期:2009年19-9]
- The synthesis of a series of conjugated spermine derivatives with benzoxadiazole, phenylxanthene or bodipy fluorophores is described. These fluorescent probes were used to identify the activity of the polyamine transport...
- Structure-activity relationships of lipopolysaccharide sequestration in N-alkylpolyamines
[作者:Shrestha, A; Sil, D; Malladi, SS; Warshakoon, HJ; David, SA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2478-2481 , 文章类型: Article,,卷期:2009年19-9]
- We have previously shown that simple N-acyl or N-alkyl polyamines bind to and sequester Gram-negative bacterial lipopolysaccharide, affording protection against lethality in animal models of endotoxicosis. Several iterat...
- Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety
[作者:Yang, SW; Ho, G; Tulshian, D; Greenlee, WJ; Tan, Z; Zhang, HT; Smith-Torhan, A; Fawzi, A; Anthes, J; Lu, S; Varty, G; Fernandez, X; McLeod, RL; Hey, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2482-2486 , 文章类型: Article,,卷期:2009年19-9]
- A series of nortropane analogs based on previously reported compound 1 have been synthesized and shown to bind to the nociceptin receptor with high affinity. The synthesis and structure-activity relationships around the ...
- Synthesis and biological evaluation of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides: A class of potent aggrecanase-1 inhibitors
[作者:Hopper, DW; Vera, MD; Howa, D; Sabatini, J; Xiang, JS; Ipek, M; Thomason, J; Hu, YH; Feyfant, E; Wang, Q; Georgiadis, KE; Reifenberg, E; Sheldon, RT; Keohan, CC; Majumdar, MK; Morris, EA; Skotnicki, J; Sum, PE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2487-2491 , 文章类型: Article,,卷期:2009年19-9]
- The prevention of aggrecan (a key component of cartilage) cleavage via the inhibition of aggrecanase-1 may provide a unique opportunity to stop the progression of cartilage degradation in osteoarthritis. The evaluation o...
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