- Synthesis and biological activity of imidazopyridine anticoccidial agents: Part II
[作者:Scribner, A; Dennis, R; Lee, SL; Ouvry, G; Perrey, D; Fisher, M; Wyvratt, M; Leavitt, P; Liberator, P; Gurnett, A; Brown, C; Mathew, J; Thompson, D; Schmatz, D; Biftu, T,期刊:European Journal of Medicinal Chemistry, 页码:1123-1151 , 文章类型: Article,,卷期:2008年43-6]
Coccidiosis is the major cause of morbidity and mortality in the poultry industry. Protozoan parasites of the genus Eimeria invade the intestinal lining of the avian host causing tissue pathology, poor weight gain, an...
- Syntheses of tetrahydroisoquinoline derivatives that inhibit NO production in activated BV-2 microglial cells
[作者:Seo, JW; Srisook, E; Son, HJ; Hwang, O; Cha, YN; Chi, DY,期刊:European Journal of Medicinal Chemistry, 页码:1160-1170 , 文章类型: Article,,卷期:2008年43-6]
Seventeen tetrahydroisoquinoline derivatives were designed, synthesized and evaluated for inhibition of NO production in lipopolysaccharide-stimulated BV-2 microglial cells. Compounds 5a, 9c and 11a potently attenuate...
- Synthesis, anti-HIV-1 integrase, and cytotoxic activities of 4-chloro-N-(4-oxopyrimidin-2-yl)-2-mercaptobenzenesulfonamide derivatives
[作者:Brzozowski, Z; Slawinski, J; Saczewski, F; Sanchez, T; Neamati, N,期刊:European Journal of Medicinal Chemistry, 页码:1188-1198 , 文章类型: Article,,卷期:2008年43-6]
Several 4-chloro-N-(4-oxopyrimidin-2-yl)-2-mercaptobenzenesulfonamide derivatives 13-28 and 35-44 have been synthesized and tested as potential HIV-1 integrase (IN) inhibitors. Compounds 15-17, 19, 21-28, 36 and 41 in...
- Novel N-(phosphonomethyl) glycine derivatives: Design, characterization and biological activity
[作者:Naydenova, ED; Todorov, PT; Topashka-Ancheva, MN; Momekov, GT; Yordanova, TZ; Konstantinov, SM; Troev, KD,期刊:European Journal of Medicinal Chemistry, 页码:1199-1205 , 文章类型: Article,,卷期:2008年43-6]
A series of C alpha,alpha-disubstituted cyclic derivatives of N-(phosphonomethyl) glycine have been synthesized and characterized. They exhibited moderate clastogenicity, low antiproliferative activity on mice bone ma...
- Comparison of the cytotoxic activities of naturally occurring hydroxyanthraquinones and hydroxynaphthoquinones
[作者:Cui, XR; Tsukada, M; Suzuki, N; Shimamura, T; Gao, L; Koyanagi, J; Komada, F; Saito, S,期刊:European Journal of Medicinal Chemistry, 页码:1206-1215 , 文章类型: Article,,卷期:2008年43-6]
Seven hydroxyanthraquinone derivatives, 1-7, were isolated from the root of Rheum palmatum (Polygonaceae). Two propionated anthraquinone derivatives, 8 and 9, were synthesized. Four hydroxynaphthoquinone derivatives, ...
- Synthesis and biological activities of a series of 4,5-diaryl-3-hydroxy-2(5H)-furanones
[作者:Bailly, F; Queffelec, C; Mbemba, G; Mouscadet, JF; Pommery, N; Pommery, J; Henichart, JP; Cotelle, P,期刊:European Journal of Medicinal Chemistry, 页码:1222-1229 , 文章类型: Article,,卷期:2008年43-6]
A series of thirteen 4,5-diaryl-3-hydroxy-2(5H)-furanones were synthesized. They were evaluated for their antioxidant potencies and inhibitory properties of 5-lipoxygenase, cyclooxygenases, HIV-1 integrase and PC3 cel...
- Design and microwave-assisted synthesis of 5-trifluoromethyl-4,5-dihydro-1H-pyrazoles: Novel agents with analgesic and anti-inflammatory properties
[作者:Sauzem, PD; Machado, P; Rubin, MA; Sant'Anna, GD; Faber, HB; de Souza, AH; Mello, CF; Beck, P; Burrow, RA; Bonacorso, HG; Zanatta, N; Martins, MAP,期刊:European Journal of Medicinal Chemistry, 页码:1237-1247 , 文章类型: Article,,卷期:2008年43-6]
In this work, we reported the synthesis and evaluation of the analgesic and anti-inflammatory properties of novel 3- or 4-substituted 5-trifluoromethyl-5-hydroxy-4,5-dihydro-1H-1-carboxyamidepyrazoles (where 3-/4-subs...
- Xanthine oxidase-activated prodrugs of thymidine phosphorylase inhibitors
[作者:Reigan, P; Gbaj, A; Stratford, IJ; Bryce, RA; Freeman, S,期刊:European Journal of Medicinal Chemistry, 页码:1248-1260 , 文章类型: Article,,卷期:2008年43-6]
Thymidine phosphorylase (TP) is over-expressed in various tumour types and plays an important role in tumour angiogenesis, growth, invasion and metastasis. The enzymatic activity of TP is required for the angiogenic e...
- Synthesis and antioxidant activity evaluation of new hexahydropyrimido[5,4-c]quinoline-2,5-diones and 2-thioxohexahydropyrimido[5,4-c]quinoline-5-ones obtained by Biginelli reaction in two steps
[作者:Ismaili, L; Nadaradjane, A; Nicod, L; Guyon, C; Xicluna, A; Robert, JF; Refouvelet, B,期刊:European Journal of Medicinal Chemistry, 页码:1270-1275 , 文章类型: Article,,卷期:2008年43-6]
New hexahydropyrimido[5,4-c]quinoline-2,5-diones and 2-thioxohexahydropyrimido [5,4-c] quinoline-5-ones were prepared in two steps from ethyl 4-phenyl-6-methyl-2-oxo tetrahydropyrimidine-5-carboxylates or 4-phenyl-6-m...
- Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases
[作者:Smaill, JB; Baker, EN; Booth, RJ; Bridges, AJ; Dickson, JM; Dobrusin, EM; Ivanovic, I; Kraker, AJ; Lee, HH; Lunney, EA; Ortwine, DF; Palmer, BD; Quin, J; Squire, CJ; Thompson, AM; Denny, WA,期刊:European Journal of Medicinal Chemistry, 页码:1276-1296 , 文章类型: Article,,卷期:2008年43-6]
A series of N-6 substituted 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones were prepared from N-substituted (5-methoxyphenyl)ethenylindoles. The target compounds were tested for their ability to inhibit t...
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