- A new class of bioactivable self-immolative N,O-ligands
[作者:Kuznik, N; Chrobaczynski, A; Mika, M; Miler, P; Komor, R; Kubicki, M,期刊:European Journal of Medicinal Chemistry, 页码:184-192 , 文章类型: Article,,卷期:2012年52-1]
- A hexadentate ligand built on an amine-bis(phenol) skeleton with an aminal, self-immolative moiety is presented. Synthesis of the ligand is convenient and relatively high yielded. Moreover, it enables synthesis of many d...
- Exploring the interplay of physicochemical properties, membrane permeability and giardicidal activity of some benzimidazole derivatives
[作者:Hernandez-Covarrubias, C; Vilchis-Reyes, MA; Yepez-Mulia, L; Sanchez-Diaz, R; Navarrete-Vazquez, G; Hernandez-Campos, A; Castillo, R; Hernandez-Luis, F,期刊:European Journal of Medicinal Chemistry, 页码:193-204 , 文章类型: Article,,卷期:2012年52-1]
- This study evaluated the relationship between the physicochemical properties, membrane permeability and in vitro giardicidal activity of twenty nine benzimidazole derivatives (1-7n). The retention time data from reverse ...
- Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization
[作者:Xie, H; Zeng, LL; Zeng, SG; Lu, X; Zhang, GC; Zhao, X; Cheng, N; Tu, ZC; Li, ZY; Xu, HJ; Yang, L; Zhang, XQ; Huang, M; Zhao, JL; Hu, WH,期刊:European Journal of Medicinal Chemistry, 页码:205-212 , 文章类型: Article,,卷期:2012年52-1]
- We previously reported a highly potent DPP-IV inhibitor 6 with low in vivo efficacy. While trying to maintain consistent in vitro and in vivo biological activity, we initiated a pharmacokinetic property-driven optimizati...
- Synthesis, cytotoxicity and apoptosis of cyclotriphosphazene compounds as anti-cancer agents
[作者:Yildirim, T; Bilgin, K; Ciftci, GY; Ecik, ET; Senkuytu, E; Uludag, Y; Tomak, L; Kilic, A,期刊:European Journal of Medicinal Chemistry, 页码:213-220 , 文章类型: Article,,卷期:2012年52-1]
- In the present study, a number of new dispirobino and dispiroansa spermine derivatives of cyclotriphosphazene (8-10, 13) were synthesized and characterized by elemental analysis, mass spectrometry, (1)H and (31)P NMR spe...
- Synthesis, characterization and biological activity of hydroxyl-bisphosphonic analogs of bile acids
[作者:Bortolini, O; Fantin, G; Fogagnolo, M; Rossetti, S; Maiuolo, L; Di Pompo, G; Avnet, S; Granchi, D,期刊:European Journal of Medicinal Chemistry, 页码:221-229 , 文章类型: Article,,卷期:2012年52-1]
- Bisphosphonates (BPs) are now the most widely used drugs for diseases associated with increased bone resorption, such as osteoporosis, and tumor bone diseases. A significant drawback of the BPs is their poor oral absorpt...
- Amino acid, dipeptide and pseudodipeptide conjugates of ring-substituted 8-aminoquinolines: Synthesis and evaluation of anti-infective, beta-haematin inhibition and cytotoxic activities
[作者:Kaur, K; Jain, M; Khan, SI; Jacob, MR; Tekwani, BL; Singh, S; Singh, PP; Jain, R,期刊:European Journal of Medicinal Chemistry, 页码:230-241 , 文章类型: Article,,卷期:2012年52-1]
- Three new series of 8-aminoquinolines with modifications in the side-chain by conjugation with amino acids, dipeptides and pseudodipeptides have been synthesized. The synthesized compounds were tested for in vitro antima...
- The conversion of oridonin to spirolactone-type or enmein-type diterpenoid: Synthesis and biological evaluation of ent-6,7-seco-oridonin derivatives as novel potential anticancer agents
[作者:Wang, L; Li, DH; Xu, ST; Cai, H; Yao, HQ; Zhang, YH; Jiang, JY; Xu, JY,期刊:European Journal of Medicinal Chemistry, 页码:242-250 , 文章类型: Article,,卷期:2012年52-1]
- Starting from commercial available natural product oridonin (1), a practical synthesis of ent-6,7-seco-oridonin derivatives (2, 3, 5, and 9) was accomplished and their biological activities were evaluated. The conversion...
- Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: Synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine
[作者:Samadi, A; de los Rios, C; Bolea, I; Chioua, M; Iriepa, I; Moraleda, I; Bartolini, M; Andrisano, V; Galvez, E; Valderas, C; Unzeta, M; Marco-Contelles, J,期刊:European Journal of Medicinal Chemistry, 页码:251-262 , 文章类型: Article,,卷期:2012年52-1]
- The synthesis, pharmacological evaluation and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amines 1-7 of type I, and 9-12 of type II, designed as multipotent inhibitors able to simultaneo...
- Design and synthesis of new 4-pyrazolin-3-yl-1,2,3-triazoles and 1,2,3-triazol-4-yl-pyrazolin-1-ylthiazoles as potential antimicrobial agents
[作者:Abdel-Wahab, BF; Abdel-Latif, E; Mohamed, HA; Awad, GEA,期刊:European Journal of Medicinal Chemistry, 页码:263-268 , 文章类型: Article,,卷期:2012年52-1]
- New pyrazolyl-1,2,3-triazoles and 1,2,3-triazol-4-yl-pyrazolylthiazoles were synthesized through multi step reactions using 1-tolylyl-4-acetyl-5-methyl-1,2,3-triazole as a precursor. All the newly synthesized compounds w...
- Synthesis, spectral characterization and antimicrobial evaluation of Schiff base Cr (III), Mn (III) and Fe (III) macrocyclic complexes
[作者:Kumar, G; Devi, S; Johari, R; Kumar, D,期刊:European Journal of Medicinal Chemistry, 页码:269-274 , 文章类型: Article,,卷期:2012年52-1]
- A Schiff base ligand was synthesized by reacting 1,4-dicarbonyl-phenyl-dihydrazide and chromene-2,3-dione (2:2) and a series of metal complexes with this new ligand were synthesized by reaction with Cr (III), Mn (III), a...
- Chemical synthesis and biological evaluation of triazole derivatives as inhibitors of InhA and antituberculosis agents
[作者:Menendez, C; Chollet, A; Rodriguez, F; Inard, C; Pasca, MR; Lherbet, C; Baltas, M,期刊:European Journal of Medicinal Chemistry, 页码:275-283 , 文章类型: Article,,卷期:2012年52-1]
- A series of triazoles have been prepared and evaluated as inhibitors of InhA as well as inhibitors of Mycobacterium tuberculosis H(37)R(v). Several of these new compounds possess a good activity against InhA, particularl...
- Rational design, synthesis and anti-proliferative properties of new CB2 selective cannabinoid receptor ligands: An investigation of the 1,8-naphthyridin-2(1H)-one scaffold
[作者:Manera, C; Saccomanni, G; Malfitano, AM; Bertini, S; Castelli, F; Laezza, C; Ligresti, A; Lucchesi, V; Tuccinardi, T; Rizzolio, F; Bifulco, M; Di Marzo, V; Giordano, A; Macchia, M; Martinelli, A,期刊:European Journal of Medicinal Chemistry, 页码:284-294 , 文章类型: Article,,卷期:2012年52-1]
- CB2 receptor ligands are becoming increasingly attractive drugs due to the potential role of this receptor in several physiopathological processes. Using our previously described series of 1,8-naphthyridin-2(1H)-on-3-car...
- Olean-18-ene triterpenoids from Celastraceae species inhibit HIV replication targeting NF-kB and Sp1 dependent transcription
[作者:Osorio, AA; Munoz, A; Torres-Romero, D; Bedoya, LM; Perestelo, NR; Jimenez, IA; Alcami, J; Bazzocchi, IL,期刊:European Journal of Medicinal Chemistry, 页码:295-303 , 文章类型: Article,,卷期:2012年52-1]
- In the present study we report the isolation of nine new olean-18-ene triterpenes (1-9), along with three known ones (10-12), from Cassine xylocarpa and Maytenus jelskii. Their stereostructures have been elucidated on th...
- On the search for potential anti-Trypanosoma cruzi drugs: Synthesis and biological evaluation of 2-hydroxy-3-methylamino and 1,2,3-triazolic naphthoquinoidal compounds obtained by click chemistry reactions
[作者:da Silva, EN; de Melo, IMM; Diogo, EBT; Costa, VA; de Souza, JD; Valenca, WO; Camara, CA; de Oliveira, RN; de Araujo, AS; Emery, FS; dos Santos, MR; de Simone, CA; Menna-Barreto, RFS; de Castro, SL,期刊:European Journal of Medicinal Chemistry, 页码:304-312 , 文章类型: Article,,卷期:2012年52-1]
- Five 2-hydroxy-3-substituted-aminomethyl naphthoquinones, nine 1,2,3-triazolic para-naphthoquinones, five nor-beta-lapachone-based 1,2,3-triazoles, and several other naphthoquinonoid compounds were synthesized and evalua...
- Cobalt, nickel, copper and zinc complexes with 1,3-diphenyl-1H-pyrazole-4-carboxaldehyde Schiff bases: Antimicrobial, spectroscopic, thermal and fluorescence studies
[作者:Singh, K; Kumar, Y; Puri, P; Kumar, M; Sharma, C,期刊:European Journal of Medicinal Chemistry, 页码:313-321 , 文章类型: Article,,卷期:2012年52-1]
- Two new Schiff bases of 1,3-diphenyl-1H-pyrazole-4-carboxaldehyde and 4-amino-5-mercapto-3-methyl/H-1,2,4-triazole [HL(1-2)] and their Cobalt, Nickel, Copper and Zinc complexes have been synthesized and characterized by ...
- Noncovalent inhibition of 20S proteasome by pegylated dimerized inhibitors
[作者:Marechal, X; Pujol, A; Richy, N; Genin, E; Basse, N; Reboud-Ravaux, M; Vidal, J,期刊:European Journal of Medicinal Chemistry, 页码:322-327 , 文章类型: Article,,卷期:2012年52-1]
- We exploited the concept of polyvalent interactions to produce highly selective and efficient inhibitors of eukaryotic proteasome. This multicatalytic protease with the unique topography of its 6 active sites has emerged...
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