- Structure activity relationship studies of 1-(4-chloro-2,5-dimethoxyphenyl)-3-(3-propoxypropyl)thiourea, a non-nucleoside reverse transcriptase inhibitor of human immunodeficiency virus type-1
[作者:Weitman, M; Lerman, K; Nudelman, A; Major, DT; Hizi, A; Herschhorn, A,期刊:European Journal of Medicinal Chemistry, 页码:447-467 , 文章类型: Article,,卷期:2011年46-2]
- The reverse transcriptase (RT) of the human immunodeficiency virus type-1 (HIV-1) is still a prime target for drug development due to the continuing need to block drug-resistant RT mutants by new inhibitors. We have prev...
- Synthesis and effects of some novel tetrahydronaphthalene derivatives on proliferation and nitric oxide production in lipopolysaccharide activated Raw 264.7 macrophages
[作者:Gurkan, AS; Karabay, AZ; Buyukbingol, Z; Buyukbingol, E,期刊:European Journal of Medicinal Chemistry, 页码:468-479 , 文章类型: Article,,卷期:2011年46-2]
- In this study, novel N-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalene-2-yl)-carboxamide (6-15) and 5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamide (16-32) derivatives were synthesized and their in v...
- Synthesis, antimicrobial activity and structure-activity relationship study of N,N-dibenzyl-cyclohexane-1,2-diamine derivatives
[作者:Sharma, M; Joshi, P; Kumar, N; Joshi, S; Rohilla, RK; Roy, N; Rawat, DS,期刊:European Journal of Medicinal Chemistry, 页码:480-487 , 文章类型: Article,,卷期:2011年46-2]
- We report herein synthesis and antimicrobial activity of a series of N,N-dibenzyl-cyclohexane-1, 2-diamine derivatives. In order to study the structure activity relationship of substituted dibenzylcyclohexane-1,2-diamine...
- Structure-based design, synthesis and preliminary anti-inflammatory activity of bolinaquinone analogues
[作者:Petronzi, C; Filosa, R; Peduto, A; Monti, MC; Margarucci, L; Massa, A; Ercolino, SF; Bizzarro, V; Parente, L; Riccio, R; de Caprariis, P,期刊:European Journal of Medicinal Chemistry, 页码:488-496 , 文章类型: Article,,卷期:2011年46-2]
- As a part of our drug discovery efforts we developed a series of simplified derivatives of bolinaquinone (BLQ), a hydroxyquinone marine metabolite, showing potent anti-inflammatory activity. Thirteen new hydroxyquinone d...
- Bismuth heterocycles based on a diphenyl sulfone scaffold: Synthesis and substituent effect on the antifungal activity against Saccharomyces cerevisiae
[作者:Murafuji, T; Fujiwara, Y; Yoshimatsu, D; Miyakawa, I; Migita, K; Mikata, Y,期刊:European Journal of Medicinal Chemistry, 页码:519-525 , 文章类型: Article,,卷期:2011年46-2]
- A series of heterocyclic organobismuth(III) compounds 2 [ClBi(5-R-C6H3-2-SO2C6H4-1'-): R = Me, Ph, MeO, Cl, H, t-Bu, CF3, F, Me2N I was synthesized in order to study the relative importance of structure and specific subs...
- Synthesis and anti-inflammatory evaluation of some new acyl-hydrazones bearing 2-aryl-thiazole
[作者:Moldovan, CM; Oniga, O; Parvu, A; Tiperciuc, B; Verite, P; Pirnau, A; Crisan, O; Bojita, M; Pop, R,期刊:European Journal of Medicinal Chemistry, 页码:526-534 , 文章类型: Article,,卷期:2011年46-2]
- This work describes recent results from our research program aiming at the synthesis and evaluation of new compounds acting as potential anti-inflammatory drugs. A series of novel acyl-hydrazones bearing 2-aryl-thiazole ...
- 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: Influence of the alkylation of position 4
[作者:Billamboz, M; Bailly, F; Lion, C; Calmels, C; Andreola, ML; Witvrouw, M; Christ, F; Debyser, Z; De Luca, L; Chimirri, A; Cotelle, P,期刊:European Journal of Medicinal Chemistry, 页码:535-546 , 文章类型: Article,,卷期:2011年46-2]
- We report herein the synthesis of a series of fifteen 2-hydroxyisoquinoline-1,3(2H,4H)-dione derivatives. Alkyl and arylalkyl groups were introduced on position 4 of the basis scaffold. All the compounds presented poor i...
- Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2
[作者:Brogi, S; Corelli, F; Di Marzo, V; Ligresti, A; Mugnaini, C; Pasquini, S; Tafi, A,期刊:European Journal of Medicinal Chemistry, 页码:547-555 , 文章类型: Article,,卷期:2011年46-2]
- This paper describes a three-dimensional quantitative structure selectivity relationships (3D-QSSR) study for selectivity of a series of ligands for cannabinoid CBI and CB2 receptors. 3D-QSSR exploration was expected to ...
- Synthesis and antibacterial evaluation of novel clarithromycin derivatives with C-4 '' elongated arylalkyl groups against macrolide-resistant strains
[作者:Ma, ST; Jiao, B; Ju, YJ; Zheng, MJ; Ma, RX; Liu, L; Zhang, L; Shen, XC; Ma, CC; Meng, Y; Wang, H; Qi, YK; Ma, XD; Cui, WP,期刊:European Journal of Medicinal Chemistry, 页码:556-566 , 文章类型: Article,,卷期:2011年46-2]
- Novel clarithromycin derivatives with C-4 '' elongated arylalkyl groups were designed, synthesized and evaluated to probe the effect of different lengths of their C-4 '' side chains on the activity against resistant bact...
- Synthesis and biological activity of pyrazolothienotetrahydroisoquinoline and [1,2,4]triazolo[3,4-a]thienotetrahydroisoquinoline derivatives
[作者:Kamal, AM; Radwan, SM; Zaki, RM,期刊:European Journal of Medicinal Chemistry, 页码:567-578 , 文章类型: Article,,卷期:2011年46-2]
- 1-Hydrazino-3-thioxo-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile (3) was subjected to react with bifunctional compounds namely: acetylacetone, ethyl cyanoacetate, ethyl benzoylactate, diethylmalonate and ethyl acetoace...
- Synthesis of 2-(aminomethyl)aziridines and their microwave-assisted ring opening to 1,2,3-triaminopropanes as novel antimalarial pharmacophores
[作者:D'hooghe, M; Kenis, S; Vervisch, K; Lategan, C; Smith, PJ; Chibale, K; De Kimpe, N,期刊:European Journal of Medicinal Chemistry, 页码:579-587 , 文章类型: Article,,卷期:2011年46-2]
- A variety of 2-(aminomethyl)aziridines was prepared and converted into the corresponding 1,2,3-triaminopropanes through a novel, microwave-assisted and regioselective ring opening by diethylamine in acetonitrile. Antipla...
- Characterization of the baicalein-bovine serum albumin complex without or with Cu2+ or Fe3+ by spectroscopic approaches
[作者:Li, DJ; Zhu, M; Xu, C; Ji, BM,期刊:European Journal of Medicinal Chemistry, 页码:588-599 , 文章类型: Article,,卷期:2011年46-2]
- The binding of baicalein to bovine serum albumin (BSA) in the absence and presence of Cu2+ or Fe3+ in aqueous solution has been studied by fluorescence, synchronous fluorescence, ultraviolet visible (UV-vis) spectra, cir...
- Synthesis and antimicrobial activity of highly functionalised novel beta-lactam grafted spiropyrrolidines and pyrrolizidines
[作者:Arumugam, N; Periyasami, G; Raghunathan, R; Kamalraj, S; Muthumary, J,期刊:European Journal of Medicinal Chemistry, 页码:600-607 , 文章类型: Article,,卷期:2011年46-2]
- A facile and one-pot synthesis of a series of novel spiropyrrolidines/pyrrolizidines with beta-lactam substituent has been accomplished through 1,3-dipolar cycloaddition reaction of alkenyl esters derived from beta-lacta...
- Anomalous behavior of pentacoordinate copper complexes of dimethylphenanthroline and derivatives of terpyridine ligands: Studies on DNA binding, cleavage and apoptotic activity
[作者:Rajalakshmi, S; Weyhermuller, T; Freddy, AJ; Vasanthi, HR; Nair, BU,期刊:European Journal of Medicinal Chemistry, 页码:608-617 , 文章类型: Article,,卷期:2011年46-2]
- Copper(II) complexes with substituted terpyridine ligands, namely [Cu(itpy)(dmp)](NO3)(2) (1) and [Cu (PtPY)(dmP)](NO3)(2) (2) have been synthesized and characterized. The interaction of the complexes with CT-DNA has bee...
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