- Synthesis and antimycobacterial activity of prodrugs of indeno[2,1-c]quinoline derivatives
[作者:Upadhayaya, RS; Shinde, PD; Kadam, SA; Bawane, AN; Sayyed, AY; Kardile, RA; Gitay, PN; Lahore, SV; Dixit, SS; Foldesi, A; Chattopadhyaya, J,期刊:European Journal of Medicinal Chemistry, 页码:1306-1324 , 文章类型: Article,,卷期:2011年46-4]
- Recently we have reported anti-TB properties of a new class of conformationally-constrained indeno[2,1-c]quinolines, which are although considerably active (MIC 0.39-0.78 mu g/mL) suffered from intense solubility problem...
- Homology modeling and structural analysis of 11 beta-hydroxysteroid dehydrogenase type 2
[作者:Yamaguchi, H; Akitaya, T; Yu, T; Kidachi, Y; Kamiie, K; Noshita, T; Umetsu, H; Ryoyama, K,期刊:European Journal of Medicinal Chemistry, 页码:1325-1330 , 文章类型: Article,,卷期:2011年46-4]
- 11 beta-hydroxysteroid dehydrogenase type 2 (11 beta HSD2) was homology-modeled by a Boltzmann-weighted randomized modeling procedure, using the X-ray crystal structure of 11 beta HSD1 (PDB code: 3HFG) as a template. The...
- 2-Acylamino-5-chlorobenzophenones with enhanced selectivity towards malaria parasites
[作者:Heinrich, S; Altenkamper, M; Bechem, B; Perruchon, J; Ortmann, R; Dahse, HM; Wang, YL; Lanzer, M; Schlitzer, M,期刊:European Journal of Medicinal Chemistry, 页码:1331-1342 , 文章类型: Article,,卷期:2011年46-4]
- Previously we described a series of 5-acylaminobenzophenones with considerable antimalarial activity. Unfortunately, most compounds also displayed high cytotoxicity resulting in low selectivity towards malaria parasites....
- Design, synthesis, and biological evaluation of novel gamma-carboline ketones as anticancer agents
[作者:Chen, J; Liu, T; Wu, R; Lou, JS; Dong, XW; He, QJ; Yang, B; Hu, YZ,期刊:European Journal of Medicinal Chemistry, 页码:1343-1347 , 文章类型: Article,,卷期:2011年46-4]
- A series of novel gamma-carboline ketones were designed, synthesized and evaluated for their cytotoxic activity in vitro against six human cancer cell lines (A549, SGC, HCT116, MCF-7, K562 and K562R). Biological evaluati...
- Synthesis and study of 2-amino-7-bromofluorenes modified with nitroxides and their precursors as dual anti-amyloid and antioxidant active compounds
[作者:Kalai, T; Petrlova, J; Balog, M; Aung, HH; Voss, JC; Hideg, K,期刊:European Journal of Medicinal Chemistry, 页码:1348-1355 , 文章类型: Article,,卷期:2011年46-4]
- A series of 2-aminofluorenes N-alkylated with nitroxides or their precursors were synthesized. The new compounds were tested on hydroxyl radical and peroxyl radical scavenging ability and inflammatory assay on the endoth...
- A comparative study of proapoptotic potential of cyano analogues of boswellic acid and 11-keto-boswellic acid
[作者:Kaur, R; Khan, S; Chib, R; Kaur, T; Sharma, PR; Singh, J; Shah, BA; Taneja, SC,期刊:European Journal of Medicinal Chemistry, 页码:1356-1366 , 文章类型: Article,,卷期:2011年46-4]
- Semi-synthetic analogues of beta-boswellic acid (BA) and 11-keto-beta-boswellic acid (MBA) were comparatively evaluated for in vitro cytotoxicity against human myeloid leukaemia (HL-60) and human cervical carcinoma (HeLa...
- Synthesis and biological activity of 2-(bis((1,3,4-oxadiazolyl/1,3,4-thiadiazolyl) methylthio)methylene)malononitriles
[作者:Padmavathi, V; Reddy, GD; Reddy, SN; Mahesh, K,期刊:European Journal of Medicinal Chemistry, 页码:1367-1373 , 文章类型: Article,,卷期:2011年46-4]
- The reactivity of ketene dithiolates in the presence of different equivalents of sodium ethoxide was studied. 2-(Bis((5-aryl-1,3,4-oxadiazol-2-yl)methylthio)methylene)malononitriles 5 and 2-(bis((5-aryl-1,3,4-thiadiazol-...
- Synthesis and evaluation of bibenzyl glycosides as potent tyrosinase inhibitors
[作者:Tajima, R; Oozeki, H; Muraoka, S; Tanaka, S; Motegi, Y; Nihei, H; Yamada, Y; Masuoka, N; Nihei, K,期刊:European Journal of Medicinal Chemistry, 页码:1374-1381 , 文章类型: Article,,卷期:2011年46-4]
- Bibenzyl glycosides 1-6 were synthesized from 2,4-dihydoxybenzaldehyde and xylose, glucose, cellobiose or maltose. The key steps in the synthesis were the Wittig reaction and trichloroacetimidate glycosylation. Tests for...
- Synthesis, biopharmaceutical characterization, antimicrobial and antioxidant activities of 1-(4 '-O-beta-D-glucopyranosyloxy-2 '-hydroxyphenyl)-3-aryl-propane-1,3-diones
[作者:Sheikh, J; Parvez, A; Juneja, H; Ingle, V; Chohan, Z; Youssoufi, M; Ben Hadda, T,期刊:European Journal of Medicinal Chemistry, 页码:1390-1399 , 文章类型: Article,,卷期:2011年46-4]
- This research communication is toward the investigation of the antibacterial, antifungal and antioxidant activities of the synthesized compounds 1-(4'-O-beta-D-glucopyranosyloxy-2'-hydroxyphenyl)-3-aryl-propane-1,3-dione...
- CORAL: Building up the model for bioconcentration factor and defining it's applicability domain
[作者:Toropov, AA; Toropova, AP; Lombardo, A; Roncaglioni, A; Benfenati, E; Gini, G,期刊:European Journal of Medicinal Chemistry, 页码:1400-1403 , 文章类型: Article,,卷期:2011年46-4]
- CORAL (CORrelation And Logic) software can be used to build up the quantitative structure - property/activity relationships (QSPR/QSAR) with optimal descriptors calculated with the simplified molecular input line entry s...
- Exploration of (S)-3-aminopyrrolidine as a potentially interesting scaffold for discovery of novel Abl and PI3K dual inhibitors
[作者:Zhang, CL; Tan, CY; Zu, XY; Zhai, X; Liu, F; Chu, BZ; Ma, XH; Chen, YZ; Gong, P; Jiang, YY,期刊:European Journal of Medicinal Chemistry, 页码:1404-1414 , 文章类型: Article,,卷期:2011年46-4]
- Based on the literature-reported compensatory effect of PI3K on Abl inhibition and the improved preclinical effect of drug combination of Abl and PI3K inhibitors, a series of compounds bearing novel scaffold of (S)-3-ami...
- Synthesis, stereochemistry, antimicrobial evaluation and QSAR studies of 2,6-diaryltetrahydropyran-4-one thiosemicarbazones
[作者:Umamatheswari, S; Balaji, B; Ramanathan, M; Kabilan, S,期刊:European Journal of Medicinal Chemistry, 页码:1415-1424 , 文章类型: Article,,卷期:2011年46-4]
- A series of 2,6-diaryltetrahydropyran-4-one thiosemicarbazones (11-27) were synthesized and characterized for evaluation of potential antibacterial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas ae...
- Synthesis and biological evaluation of some 4-functionalized-pyrazoles as antimicrobial agents
[作者:Sharma, PK; Chandak, N; Kumar, P; Sharma, C; Aneja, KR,期刊:European Journal of Medicinal Chemistry, 页码:1425-1432 , 文章类型: Article,,卷期:2011年46-4]
- 1,3-Diaryl-4-formylpyrazoles 8 bearing benzenesulfonamide moiety at position-1 were synthesized as important intermediates following Vilsmeier-Haack strategy. Aldehyde moiety of 4-formylpyrazole was then converted into c...
- A facile, one-pot synthesis, characterization and antimicrobial activity of o-hydroxy anilide derivatives and 1-substituted-1,3-dicyclohexylurea analogs of long chain carboxylic acids
[作者:Farshori, NN; Ahmad, A; Khan, AU; Rauf, A,期刊:European Journal of Medicinal Chemistry, 页码:1433-1438 , 文章类型: Article,,卷期:2011年46-4]
- A series of novel o-hydroxy anilide derivatives and 1-substituted-1,3-dicyclohexylurea analogs of long chain carboxylic acids have been synthesized. The structures of the synthesized compounds were elucidated by IR, H-1 ...
- Synthesis and biological evaluation of indazole derivatives
[作者:Claramunt, RM; Lopez, C; Lopez, A; Perez-Medina, C; Perez-Torralba, M; Alkorta, I; Elguero, J; Escames, G; Acuna-Castroviejo, D,期刊:European Journal of Medicinal Chemistry, 页码:1439-1447 , 文章类型: Article,,卷期:2011年46-4]
- The inhibition of neuronal and inducible nitric oxide synthases (nNOS and iNOS) by a series of 36 indazoles has been evaluated, showing that most of the assayed derivatives are better iNOS than nNOS inhibitors. A parabol...
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