- Discovery of a small molecule inhibitor through interference with the gp120-CD4 interaction
[作者:Williams, DH; Adam, F; Fenwick, DR; Fok-Seang, J; Gardner, I; Hay, D; Jaiessh, R; Middleton, DS; Mowbray, CE; Parkinson, T; Perros, M; Pickford, C; Platts, M; Randall, A; Siddle, D; Stephenson, PT; Tran, TD; Vuong, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5246-5249 , 文章类型: Article,,卷期:2009年19-17]
- A series of piperazine derivatives were designed and synthesised as gp120-CD4 inhibitors. SAR studies led to the discovery of potent inhibitors in a cell based anti viral assay represented by compounds 9 and 28. The rat ...
- Design and optimisation of potent gp120-CD4 inhibitors
[作者:Tran, TD; Adam, FM; Calo, F; Fenwick, DR; Fok-Seang, J; Gardner, I; Hay, DA; Perros, M; Rawal, J; Middleton, DS; Parkinson, T; Pickford, C; Platts, M; Randall, A; Stephenson, PT; Vuong, H; Williams, DH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5250-5255 , 文章类型: Article,,卷期:2009年19-17]
- The synthesis and structure-activity relationship of a series of novel gp120-CD4 inhibitors are described. Pharmacokinetic studies and antiviral spectrum assessment of lead compounds led to the identification of compound...
- Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration
[作者:Woodrow, MD; Ballantine, SP; Barker, MD; Clarke, BJ; Dawson, J; Dean, TW; Delves, CJ; Evans, B; Gough, SL; Guntrip, SB; Holman, S; Holmes, DS; Kranz, M; Lindvaal, MK; Lucas, FS; Neu, M; Ranshaw, LE; Solanke, YE; Somers, DO; Ward, P; Wiseman, JO,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5261-5265 , 文章类型: Article,,卷期:2009年19-17]
- Crystallography driven optimisation of a lead derived from similarity searching of the GSK compound collection resulted in the discovery of quinoline-3-carboxamides as highly potent and selective inhibitors of phosphodie...
- Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors
[作者:Lacombe, P; Chauret, N; Claveau, D; Day, S; Deschenes, D; Dube, D; Gallant, M; Girard, Y; Huang, Z; Laliberte, F; Levesque, JF; Liu, S; Macdonald, D; Mancini, JA; Masson, P; Nicholson, DW; Nicoll-Griffith, DA; Salem, M; Styhler, A; Young, RN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5266-5269 , 文章类型: Article,,卷期:2009年19-17]
- Substituted 8-arylquinoline analogs bearing alkyl-linked side chain were identified as potent inhibitors of type 4 phophodiesterase. These compounds address the potential liabilities of the clinical candidate L454560. Th...
|