- Optimization of a series of multi-isoform PI3 kinase inhibitors
[作者:Perry, B; Beevers, R; Bennett, G; Buckley, G; Crabbe, T; Gowers, L; James, L; Jenkins, K; Lock, C; Sabin, V; Wright, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5299-5302 , 文章类型: Article,,卷期:2008年18-19]
- Optimization of the cellular and pharmacological activity of a novel series of PI3 kinase inhibitors targeting multiple isoforms is described. (c) 2008 Elsevier Ltd. All rights reserved.
- Designing rapid onset selective serotonin re-uptake inhibitors. Part 3: Site-directed metabolism as a strategy to avoid active circulating metabolites: Structure-activity relationships of (thioalkyl) phenoxy benzylamines
[作者:Middleton, DS; Andrews, M; Glossop, P; Gymer, G; Hepworth, D; Jessiman, A; Johnson, PS; MacKenny, M; Stobie, A; Tang, K; Morgan, P; Jones, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5303-5306 , 文章类型: Article,,卷期:2008年18-19]
- A series of thio-alkyl containing diphenylethers were designed and evaluated, as a strategy to competitively direct metabolism away from unwanted amine N-demethylation and deliver a pharmacologically inactive S-oxide met...
- Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase
[作者:Melamed, JY; Egbertson, MS; Varga, S; Vacca, JP; Moyer, G; Gabryelski, L; Felock, PJ; Stillmock, KA; Witmer, MV; Schleif, W; Hazuda, DJ; Leonard, Y; Jin, LX; Ellis, JD; Young, SD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5307-5310 , 文章类型: Article,,卷期:2008年18-19]
- HIV-1 integrase catalyzes the insertion of viral DNA into the genome of the host cell. Integrase inhibitor N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide selectively inhibits the strand transfer process of ...
- Modification of the side chain of micromolide, an anti-tuberculosis natural product
[作者:Yuan, H; He, R; Wan, BJ; Wang, YH; Pauli, GF; Franzblau, SG; Kozikowski, AP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5311-5315 , 文章类型: Article,,卷期:2008年18-19]
- This paper describes a series of modi. cations of the side chain of micromolide, an anti-tuberculosis natural product. Most of the synthesized compounds showed significantly decreased activities, which suggests that the ...
- Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels
[作者:Gentles, RG; Grant-Young, K; Hu, SH; Huang, YZ; Poss, MA; Andres, C; Fiedler, T; Knox, R; Lodge, N; Weaver, CD; Harden, DG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5316-5319 , 文章类型: Article,,卷期:2008年18-19]
- An initial SAR study on a series of apamin-displacing 2-aminothiazole K(Ca)2 channel blockers is described. Potent inhibitors such as N-(4-methylpyridin-2-yl)-4-(pyridin-2-yl) thiazol-2-amine (13) are disclosed, and for ...
- Structure-activity relationships of compounds targeting mycobacterium tuberculosis 1-deoxy-D-xylulose 5-phosphate synthase
[作者:Mao, JL; Eoh, HJ; He, R; Wang, YH; Wan, BJ; Franzblau, SG; Crick, DC; Kozikowski, AP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5320-5323 , 文章类型: Article,,卷期:2008年18-19]
- We report on a target- based approach to identify possible Mycobacterium tuberculosis DXS inhibitors from the structure of a known transketolase inhibitor. A small focused library of analogs was assembled in order to beg...
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