- Synthesis and biological evaluation of 3,6-disubstituted [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as a novel class of potential anti-tumor agents
[作者:Ibrahim, DA,期刊:European Journal of Medicinal Chemistry, 页码:2776-2781 , 文章类型: Article,,卷期:2009年44-7]
A new series of 3,6-disubstituted triazolo[3,4-b]thiadiazole derivatives have been synthesized by simple, high yielding routes. The key step in the construction of the triazolo[3,4-d]thiadiazole nucleus involves the r...
- Synthesis, antifungal activities and 3D-QSAR study of N-(5-substituted-1,3, 4-thiadiazol-2-yl)cyclopropanecarboxamides
[作者:Liu, XH; Shi, YX; Ma, Y; Zhang, CY; Dong, WL; Pan, L; Wang, BL; Li, BJ; Li, ZM,期刊:European Journal of Medicinal Chemistry, 页码:2782-2786 , 文章类型: Article,,卷期:2009年44-7]
- A series of cyclopropanecarboxamide were prepared and tested for antifungal activity in vivo. The preliminary bioassays indicated that some compounds are comparable to the commercial fungicides. To further explore the co...
- Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit
[作者:Zbinden, KG; Anselm, L; Banner, DW; Benz, J; Blasco, F; Decoret, G; Himber, J; Kuhn, B; Panday, N; Ricklin, F; Risch, P; Schlatter, D; Stahl, M; Thomi, S; Unger, R; Haap, W,期刊:European Journal of Medicinal Chemistry, 页码:2787-2795 , 文章类型: Article,,卷期:2009年44-7]
- Starting from a hit identified by focused screening, 3-aminopyrrolidine factor Xa inhibitors were designed. The binding mode as determined by X-ray structural analysis as well as the pharmacokinetic behaviour of selected...
- Synthesis and evaluation of a novel series of heterocyclic oleanolic acid derivatives with anti-osteoclast formation activity
[作者:Li, JF; Zhao, Y; Cai, MM; Li, XF; Li, JX,期刊:European Journal of Medicinal Chemistry, 页码:2796-2806 , 文章类型: Article,,卷期:2009年44-7]
- Oleanolic acid with anti-bone resorption effect was an active component discovered in a medicinal plant of Achyranthes bidentata. A series of heterocyclic derivatives of oleanolic acid including indole, pyrazine, quinoxa...
- Synthesis, characterisation and in vitro cytotoxicity studies of a series of chiral platinum(II) complexes based on the 2-aminomethylpyrrolidine ligand: X-ray crystal structure of [PtCl2(R-dimepyrr)] (R-dimepyrr = N-dimethyl-2(R)-aminomethylpyrrolidine)
[作者:Diakos, CI; Zhang, M; Beale, PJ; Fenton, RR; Hambley, TW,期刊:European Journal of Medicinal Chemistry, 页码:2807-2814 , 文章类型: Article,,卷期:2009年44-7]
- A series of platinum(II) complexes were synthesised based on the enantiomerically pure amino acid proline. Novel synthetic pathways were developed, adapted from standard peptide chemistry, to produce the 2-aminomethylpyr...
- Synthesis and biological evaluation of a novel series of 1,5-benzothiazepine derivatives as potential antimicrobial agents
[作者:Wang, LZ; Zhang, P; Zhang, XM; Zhang, YH; Li, Y; Wang, YX,期刊:European Journal of Medicinal Chemistry, 页码:2815-2821 , 文章类型: Article,,卷期:2009年44-7]
- Two series of novel 1,5-benzothiazepine derivatives (23 compounds) were efficiently synthesized and evaluated for antibacterial and antifungal activities. The results indicated that the compounds possessed a broad spectr...
- Synthesis and antimicrobial studies of novel methylene bridged benzisoxazolyl imidazo[2,1-b][1,3,4]thiadiazole derivatives
[作者:Lamani, RS; Shetty, NS; Kamble, RR; Khazi, IAM,期刊:European Journal of Medicinal Chemistry, 页码:2828-2833 , 文章类型: Article,,卷期:2009年44-7]
- Novel methylene bridged benzisoxazolyl imidazo[2,1-b][1,3,4]thiadiazoles (3a-f) were synthesized from benzisoxazolyl-3-acetic acid and thiosemicarbazide. Reaction of 3 with bromine in glacial acetic acid in the presence ...
- Synthesis, pharmacological and in silico evaluation of 1-(4-di-hydroxy-3,5-dioxa-4-borabicyclo[4.4.0]deca-7,9,11-trien-9-yl)-2-(tert-butylamino)ethanol, a compound designed to act as a beta(2) adrenoceptor agonist
[作者:Soriano-Ursua, MA; Valencia-Hernandez, I; Arellano-Mendoza, MG; Correa-Basurto, J; Trujillo-Ferrara, JG,期刊:European Journal of Medicinal Chemistry, 页码:2840-2846 , 文章类型: Article,,卷期:2009年44-7]
- In this study, 1-(4-di-hydroxy-3,5-dioxa-4-borabicyclo[4.4.0]deca-7,9,11-trien-9-yl)-2-(tert-butylamino)ethanol, (BR-AEA), was designed, synthesized, characterized and tested in docking studies and in vitro. Previous to ...
- DNA-targeting pyrroloquinoline-linked butenone and chalcones: Synthesis and biological evaluation
[作者:Via, LD; Gia, O; Chiarelotto, G; Ferlin, MG,期刊:European Journal of Medicinal Chemistry, 页码:2854-2861 , 文章类型: Article,,卷期:2009年44-7]
- A series of conjugates of alpha,beta-unsaturated ketone systems, phenyl-butenone and diaryl-propenones (chalcones), with the tricyclic planar pyrroloquinoline nucleus were synthesised and evaluated for their anticancer p...
- Arginine vasopressin and its analogues - The influence of position 2 modification with 3,3-diphenylalanine enantiomers. Highly potent V-2 agonists
[作者:Kwiatkowska, A; Sobolewski, D; Prahl, A; Borovickova, L; Slaninova, J; Lammek, B,期刊:European Journal of Medicinal Chemistry, 页码:2862-2867 , 文章类型: Article,,卷期:2009年44-7]
- Eleven new analogues of arginine vasopressin (AVP) modified in position 2 by 3,3-diphenyl-L-alanine or its D-enantiomer (Dip or D-Dip) were synthesized and pharmacologically evaluated for their pressor, antidiuretic and ...
- 3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment
[作者:Chen, YD; Li, FF; Tang, WQ; Zhu, CC; Jiang, YJ; Zou, JW; Yu, QS; You, QD,期刊:European Journal of Medicinal Chemistry, 页码:2868-2876 , 文章类型: Article,,卷期:2009年44-7]
- Histone deacetylases (HDACs) enzyme is a promising target for the development of anticancer drugs. The enzyme-bound conformation of Trichostatin A (TSA) (PDB ID:1C3R) as an inhibitor of HDACs was used to manually constru...
- Synthesis and evaluation of pyrido[1,2-a]pyrimidines as inhibitors of nitric oxide synthases
[作者:Bluhm, U; Boucher, JL; Buss, U; Clement, B; Friedrich, F; Girreser, U; Heber, D; Lam, T; Lepoivre, M; Rostaie-Gerylow, M; Wolschendorf, U,期刊:European Journal of Medicinal Chemistry, 页码:2877-2887 , 文章类型: Article,,卷期:2009年44-7]
- A series of new 3-aroylpyrido[1,2-a]pyrimidines were synthesized from aryl methyl ketones in a simple two-step procedure and evaluated as nitric oxide synthases (NOS) inhibitors. In order to perform a structure-activity ...
- 3D-QSAR studies on the inhibitors of AP-1 and NF-kappa B mediated transcriptional activation
[作者:Qin, J; Liu, HX; Li, JZ; Ren, YY; Yao, XJ; Liu, M,期刊:European Journal of Medicinal Chemistry, 页码:2888-2895 , 文章类型: Article,,卷期:2009年44-7]
- Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were performed on a series of 68 inhibitors of AP-1 and NF-kappa B mediated transcriptional activations. The CoM...
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