- Molecular mechanism of serotonin transporter inhibition elucidated by a new flexible docking protocol
[作者:Gabrielsen, M; Kurczab, R; Ravna, AW; Kufareva, I; Abagyan, R; Chilmonczyk, Z; Bojarski, AJ; Sylte, I,期刊:European Journal of Medicinal Chemistry, 页码:24-37 , 文章类型: Article,,卷期:2012年47-1]
- The two main groups of antidepressant drugs, the tricyclic antidepressants (TCAs) and the selective serotonin reuptake inhibitors (SSRIs), as well as several other compounds, act by inhibiting the serotonin transporter (...
- Molecular docking of gamma-sitosterol with some targets related to diabetes
[作者:Balamurugan, R; Stalin, A; Ignacimuthu, S,期刊:European Journal of Medicinal Chemistry, 页码:38-43 , 文章类型: Article,,卷期:2012年47-1]
- gamma-sitosterol isolated from Lippia nodiflora was taken as ligand for molecular docking. The molecular targets, glucokinase, Fructose 1, 6- bisphosphatase 1, Human multidrug resistance protein 1 and Cytochromes P450 wh...
- Synthesis, anti-inflammatory activity and molecular docking studies of 2,5-diarylfuran amino acid derivatives
[作者:Stefani, HA; Botteselle, GV; Zukerman-Schpector, J; Caracelli, I; Correa, DD; Farsky, SHP; Machado, ID; Santin, JR; Hebeda, CB,期刊:European Journal of Medicinal Chemistry, 页码:52-58 , 文章类型: Article,,卷期:2012年47-1]
- A series of 2,5-diaryl substituted furans functionalized with several amino acids were synthesized and evaluated as the cyclooxygenases COX-1 and COX-2 enzymes inhibitors. The proline-substituted compound inhibited PGE(2...
- Cyclosulfamide-based derivatives as inhibitors of noroviruses
[作者:Dou, D; Mandadapu, SR; Alliston, KR; Kim, Y; Chang, KO; Groutas, WC,期刊:European Journal of Medicinal Chemistry, 页码:59-64 , 文章类型: Article,,卷期:2012年47-1]
- An optimization campaign focused on improving pharmacological activity and physicochemical properties of a recently-identified class of cyclosulfamide-based norovirus inhibitors has been carried out. Dimeric compound 4 w...
- Substituted thiazoles V. Synthesis and antitumor activity of novel thiazolo[2,3-b]quinazoline and pyrido[4,3-d]thiazolo[3,2-a]pyrimidine analogues
[作者:Al-Omary, FAM; Hassan, GS; El-Messery, SM; El-Subbagh, HI,期刊:European Journal of Medicinal Chemistry, 页码:65-72 , 文章类型: Article,,卷期:2012年47-1]
- A novel series of thiazolo[2,3-b]quinazoline (14-23, 26 and 27), and pyrido[4,3-d]thiazolo[3,2-a] pyrimidine (34-43, 45 and 46) analogues were designed and synthesized. The obtained compounds were evaluated for their in-...
- Synthesis, crystal structure and pharmacological evaluation of two new Cu(II) complexes of 2-oxo-1,2-dihydroquinoline-3-carbaldehyde (benzoyl) hydrazone: A comparative investigation
[作者:Raja, DS; Bhuvanesh, NSP; Natarajan, K,期刊:European Journal of Medicinal Chemistry, 页码:73-85 , 文章类型: Article,,卷期:2012年47-1]
- Two new copper(II) complexes have been synthesized by reacting 2-oxo-1,2-dihydroquinoline-3-carbaldehyde (benzoyl) hydrazone (H(2)L) with CuCl(2)center dot 2H(2)O or Cu(NO(3))(2)center dot 3H(2)O. The structures of the c...
- Anti-AIDS agents 85. Design, synthesis, and evaluation of 1R,2R-dicamphanoyl-3,3-dimethyldihydropyrano-[2,3-c]xanthen-7(1H)-one (DCX) derivatives as novel anti-HIV agents
[作者:Zhou, T; Shi, Q; Chen, CH; Huang, L; Ho, P; Morris-Natschke, SL; Lee, KH,期刊:European Journal of Medicinal Chemistry, 页码:86-96 , 文章类型: Article,,卷期:2012年47-1]
- In this study, 1R,2R-dicamphanoyl-3,3-dimethydihydropyrano[2,3-c]xanthen-7(1H)-one (DCX) derivatives were designed and synthesized as novel anti-HIV agents against both wild-type and non-nucleoside reverse transcriptase ...
- Bis-chalcone analogues as potent NO production inhibitors and as cytotoxic agents
[作者:Reddy, MVB; Shen, YC; Ohkoshi, E; Bastow, KF; Qian, K; Lee, KH; Wu, TS,期刊:European Journal of Medicinal Chemistry, 页码:97-103 , 文章类型: Article,,卷期:2012年47-1]
- Chalcones have a distinctive 1,3-diarylpropenone skeleton and exert numerous biological effects. Using a one-step Claisen-Schmidt condensation, we synthesized eleven bis-chalcones (3-13) and three acetyl chalcones (14-16...
- 1,2,4-Triazole D-ribose derivatives: Design, synthesis and antitumoral evaluation
[作者:Avanzo, RE; Anesini, C; Fascio, ML; Errea, MI; D'Accorso, NB,期刊:European Journal of Medicinal Chemistry, 页码:104-110 , 文章类型: Article,,卷期:2012年47-1]
- Herein we report the design, synthesis and characterization of novel 1,2,4-triazole D-ribose derivatives, as well as their synthetic precursors.The antitumoral activity against T cell lymphoma cell line of these products...
- Fragment-based design, docking, synthesis, biological evaluation and structure-activity relationships of 2-benzo/benzisothiazolimino-5-aryliden-4-thiazolidinones as cycloxygenase/lipoxygenase inhibitors
[作者:Eleftheriou, P; Geronikaki, A; Hadjipavlou-Litina, D; Vicini, P; Filz, O; Filimonov, D; Poroikov, V; Chaudhaery, SS; Roy, KK; Saxena, AK,期刊:European Journal of Medicinal Chemistry, 页码:111-124 , 文章类型: Article,,卷期:2012年47-1]
- Balanced modulation of several targets is one of the current strategies for the treatment of multi-factorial diseases. Based on the knowledge of inflammation mechanisms, it was inferred that the balanced inhibition of cy...
- 3,5-Disubstituted-thiazolidine-2,4-dione analogs as anticancer agents: Design, synthesis and biological characterization
[作者:Liu, K; Rao, W; Parikh, H; Li, QB; Guo, TL; Grant, S; Kellogg, GE; Zhang, SJ,期刊:European Journal of Medicinal Chemistry, 页码:125-137 , 文章类型: Article,,卷期:2012年47-1]
- A series of 2,5-disubstituted-thiazolidine-2,4-dione analogs based on the newly identified lead 1, a potential anticancer agent via the inhibition of the Raf/MEK/extracellular signal regulated kinase (ERK) and phosphatid...
- Synthesis and biological activity of dihydroimidazole and 3,4-dihydrobenzo[4,5]imidazo[1,2-a][1,3,5]triazins
[作者:Soliman, AM; Mohamed, SK; El Remaily, MAA; Abdel-Ghany, H,期刊:European Journal of Medicinal Chemistry, 页码:138-142 , 文章类型: Article,,卷期:2012年47-1]
- Reaction of 2-guanidinobenzimidazole with halogenated active methylenes and ketones gave dihydroimidazole and 3,4-dihydrobenzo[4,5]imidazo [1,2-a][1,3,5]triazin derivatives in very good yield. The anti-bacterial evaluati...
- Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: A first round of lead optimization
[作者:La Pietra, V; Marinelli, L; Cosconati, S; Di Leva, FS; Nuti, E; Santamaria, S; Pugliesi, I; Morelli, M; Casalini, F; Rossello, A; La Motta, C; Taliani, S; Visse, R; Nagase, H; da Settimo, F; Novellino, E,期刊:European Journal of Medicinal Chemistry, 页码:143-152 , 文章类型: Article,,卷期:2012年47-1]
- Osteoarthritis (OA) is the leading cause of joint pain and disability in middle-aged and elderly patients, and is characterized by progressive loss of articular cartilage. Among the various matrix metalloproteinases (MMP...
- Synthesis and evaluation of the substrate activity of C-6 substituted purine ribosides with E. coli purine nucleoside phosphorylase: Palladium mediated cross-coupling of organozinc halides with 6-chloropurine nucleosides [1]
[作者:Hassan, AEA; Abou-Elkhair, RAI; Riordan, JM; Allan, PW; Parker, WB; Khare, R; Waud, WR; Montgomery, JA; Secrist, JA,期刊:European Journal of Medicinal Chemistry, 页码:167-174 , 文章类型: Article,,卷期:2012年47-1]
- A series of C-6 alkyl, cycloalkyl, and aryl-9-(beta-D-ribofuranosyl)purines were synthesized and their substrate activities with Escherichia colt purine nucleoside phosphorylase (E. coli PNP) were evaluated. (Ph(3)P)(4)P...
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