- Novel sulfonylurea derivatives as H(3) receptor antagonists. Preliminary SAR studies
[作者:Ceras, J; Cirauqui, N; Perez-Silanes, S; Aldana, I; Monge, A; Galiano, S,期刊:European Journal of Medicinal Chemistry, 页码:1-13 , 文章类型: Article,,卷期:2012年52-1]
- The combination of antagonism at histamine H(3) receptor and the stimulation of insulin secretion have been proposed as an approach to new dual therapeutic agents for the treatment of type 2 diabetes mellitus associated ...
- Conformationnally restricted naphthalene derivatives type isocombretastatin A-4 and isoerianin analogues: Synthesis, cytotoxicity and antitubulin activity
[作者:Rasolofonjatovo, E; Provot, O; Hamze, A; Rodrigo, J; Bignon, J; Wdzieczak-Bakala, J; Desravines, D; Dubois, J; Brion, JD; Alami, M,期刊:European Journal of Medicinal Chemistry, 页码:22-32 , 文章类型: Article,,卷期:2012年52-1]
- A novel series of dihydronaphtalene, tetrahydronaphtalene and naphtalene derivatives as restricted analogues of isoCA-4 were designed, synthesized and evaluated for their anticancer properties. High cell growth inhibitio...
- Discovery of flavonoid derivatives as anti-HCV agents via pharmacophore search combining molecular docking strategy
[作者:Liu, MM; Zhou, L; He, PL; Zhang, YN; Zhou, JY; Shen, Q; Chen, XW; Zuo, JP; Li, W; Ye, DY,期刊:European Journal of Medicinal Chemistry, 页码:33-43 , 文章类型: Article,,卷期:2012年52-1]
- Common feature based pharmacophore and structure-based docking approaches have been employed in the identification of novel anti-HCV candidates from our in-house database. A total of 31 hits identified in silico were scr...
- Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives
[作者:Audisio, D; Messaoudi, S; Cojean, S; Peyrat, JF; Brion, JD; Bories, C; Huteau, F; Loiseau, PM; Alami, M,期刊:European Journal of Medicinal Chemistry, 页码:44-50 , 文章类型: Article,,卷期:2012年52-1]
- A new family of quinolinone derivatives has been synthesized and evaluated for their antikinetoplastid activities against Leishmania donovani and Trypanosoma brucei brucei. Results from these structure activity relations...
- 2-Aminothiophenes as building blocks in heterocyclic synthesis: Synthesis and antimicrobial evaluation of a new class of pyrido[1,2-a]thieno[3,2-e]pyrimidine, quinoline and pyridin-2-one derivatives
[作者:Behbehani, H; Ibrahim, HM; Makhseed, S; Elnagdi, MH; Mahmoud, H,期刊:European Journal of Medicinal Chemistry, 页码:51-65 , 文章类型: Article,,卷期:2012年52-1]
- Multisubstituted 2-aminothiophenes la c can be readily cyanoacylated via reaction with cyanoacetic acid in presence of acetic anhydride under a microwave irradiation to form the corresponding cyanoacetamides 2a-c, which ...
- In vitro antimycoplasmal activity of citrus bergamia essential oil and its major components
[作者:Furneri, PM; Mondello, L; Mandalari, G; Paolino, D; Dugo, P; Garozzo, A; Bisignano, G,期刊:European Journal of Medicinal Chemistry, 页码:66-69 , 文章类型: Article,,卷期:2012年52-1]
- Forty-two strains of Mycoplasma hominis (including PG21), 2 strain of Mycoplasma fermentans (Pg18 and K7), 1 strain of Mycoplasma pneumoniae (strain m129) were investigated for their susceptibilities to Citrus bergamia e...
- Design, synthesis and biological evaluation of thiazole- and indole-based derivatives for the treatment of type II diabetes
[作者:Xu, QY; Huang, L; Liu, J; Ma, L; Chen, T; Chen, JY; Peng, F; Cao, D; Yang, Z; Qiu, N; Qiu, JX; Wang, GC; Liang, XL; Peng, AH; Xiang, ML; Wei, YQ; Chen, LJ,期刊:European Journal of Medicinal Chemistry, 页码:70-81 , 文章类型: Article,,卷期:2012年52-1]
- Present studies have shown that the lipid carrier has a significant role in several aspects of metabolic syndrome in A-FABP/ap2-deficient mice, including type 2 diabetes and atherosclerosis. 38 Thiazole- and indole-based...
- 2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies
[作者:Singh, K; Kaur, H; Chibale, K; Balzarini, J; Little, S; Bharatam, PV,期刊:European Journal of Medicinal Chemistry, 页码:82-97 , 文章类型: Article,,卷期:2012年52-1]
- 2-Aminopyrimidine based 4-aminoquinolines were synthesized using an efficacious protocol. Some of the compounds showed in vitro anti-plasmodial activity against drug-sensitive CQ(S) (3D7) and drug-resistant CQ(R) (K1) st...
- A novel series of L-2-benzyloxycarbonylamino-8-(2-pyridyl)-disulfidyloctanoic acid derivatives as histone deacetylase inhibitors: Design, synthesis and molecular modeling study
[作者:Huang, DW; Li, XH; Wei, YD; Xiu, ZL,期刊:European Journal of Medicinal Chemistry, 页码:111-122 , 文章类型: Article,,卷期:2012年52-1]
- Histone deacetylases inhibitors (HDACIs) have become an attractive class of anticancer agents. In order to find some novel potent HDACIs, we designed and synthesized a series of L-2-benzyloxycarbonylamino-8-(2-pyridyl)-d...
- Design, synthesis, and antitumor evaluation of 2,4,6-triaryl pyridines containing chlorophenyl and phenolic moiety
[作者:Thapa, P; Karki, R; Yun, M; Kadayat, TM; Lee, E; Kwon, HB; Na, Y; Cho, WJ; Kim, ND; Jeong, BS; Kwon, Y; Lee, ES,期刊:European Journal of Medicinal Chemistry, 页码:123-136 , 文章类型: Article,,卷期:2012年52-1]
- We have designed and synthesized a series of 2,4,6-triaryl pyridine derivatives containing chlorophenyl and phenolic moeity at 2- and 4- position of the central pyridine, respectively, resulting in a total of 42 compound...
- Imidazonaphthyridine systems (part 2): Functionalization of the phenyl ring linked to the pyridine pharmacophore and its replacement by a pyridinone ring produces intriguing differences in cytocidal activity
[作者:Masurier, N; Debiton, E; Jacquemet, A; Bussiere, A; Chezal, JM; Ollivier, A; Tetegan, D; Andaloussi, M; Galmier, MJ; Lacroix, J; Canitrot, D; Teulade, JC; Gaudreault, RC; Chavignon, O; Moreau, E,期刊:European Journal of Medicinal Chemistry, 页码:137-150 , 文章类型: Article,,卷期:2012年52-1]
- We recently discovered that five- and pseudo-five-fused-ring derivatives in an imidazonaphthyridine series were promising hit compounds for the development of new DNA-intercalators. In this study, novel (dihydro)imidazo[...
- Synthesis, structure-activity relationship and in vitro anti-mycobacterial evaluation of 13-n-octylberberine derivatives
[作者:Liu, YX; Xiao, CL; Wang, YX; Li, YH; Yang, YH; Li, YB; Bi, CW; Gao, LM; Jiang, JD; Song, DQ,期刊:European Journal of Medicinal Chemistry, 页码:151-158 , 文章类型: Article,,卷期:2012年52-1]
- Twenty-eight new 13-n-octylberberine derivatives were synthesized and evaluated for their activities against drug-susceptible Mycobacterium tuberculosis (M. tuberculosis) strain H(37)Rv. Among these compounds, compound 1...
- Novel pH-sensitive cationic lipids with linear ortho ester linkers for gene delivery
[作者:Chen, HG; Zhang, HZ; Thor, D; Rahimian, R; Guo, X,期刊:European Journal of Medicinal Chemistry, 页码:159-172 , 文章类型: Article,,卷期:2012年52-1]
- In an effort to develop pH-sensitive lipoplexes for efficient gene delivery, we report three novel cationic lipids containing a linear ortho ester linker that conjugates either the headgroup (Type I) or one hydrocarbon c...
- GnRH-III based multifunctional drug delivery systems containing daunorubicin and methotrexate
[作者:Leurs, U; Lajko, E; Mezo, G; Orban, E; Ohlschlager, P; Marquardt, A; Kohidai, L; Manea, M,期刊:European Journal of Medicinal Chemistry, 页码:173-183 , 文章类型: Article,,卷期:2012年52-1]
- Here we report on the design, synthesis and biochemical characterization of multifunctional bio-conjugates containing two chemotherapeutic agents, daunorubicin and methotrexate, coupled to the GnRH-III decapeptide, which...
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