- Design, synthesis and biological evaluation of novel 2-[(2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ylidene)hydrazono]-1,3-thiazolidin-4-ones as a new class of antimicrobial agents
[作者:Ramachandran, R; Rani, M; Kabilan, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2819-2823 , 文章类型: Article,,卷期:2009年19-10]
- New series of 2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-one thiosemicarbazones (9-16) obtained from the corresponding 2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ones (1-8) upon cyclization with ethylbromoacetate in the presence o...
- Surface plasmon resonance-based detection of ladder-shaped polyethers by inhibition detection method
[作者:Mouri, R; Oishi, T; Torikai, K; Ujihara, S; Matsumori, N; Murata, M; Oshima, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2824-2828 , 文章类型: Article,,卷期:2009年19-10]
- Ladder-shaped polyether (LSP) compounds represented by brevetoxins and ciguatoxins were largely discovered in association with seafood poisoning. Thus, a quick quantification method for LSPs is potentially important. We ...
- 4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: Design, synthesis and structure-activity relationships
[作者:Fish, PV; Andrews, MD; Fray, MJ; Stobie, A; Wakenhut, F; Whitlock, GA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2829-2834 , 文章类型: Article,,卷期:2009年19-10]
- Single enantiomer [(aryloxy)(pyridinyl) methyl] piperidine and pyrrolidine derivatives 5-9 are inhibitors of monoamine reuptake. Structure-activity relationships established that monoamine reuptake inhibition are functio...
- Identification and characterization of a selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R)
[作者:Ito, M; Sakamoto, T; Suzuki, T; Egashira, S; Moriya, M; Ishihara, A; Iwaasa, H; Matsushita, H; Nakase, K; Wallace, MA; Dean, D; Sato, N; Tokita, S; Kanatani, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2835-2839 , 文章类型: Article,,卷期:2009年19-10]
- We have developed and characterized [S-35]4a as a potent and selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R). Compound [S-35]4a showed appreciable specific signals in brain slices prepared from...
- Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors
[作者:Giannini, G; Marzi, M; Di Marzo, M; Battistuzzi, G; Pezzi, R; Brunetti, T; Cabri, W; Vesci, L; Pisano, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2840-2843 , 文章类型: Article,,卷期:2009年19-10]
- In order to gather further knowledge about the structural requirements on histone deacetylase inhibitors (HDACi), starting from the schematic model of the common pharmacophore that characterizes this class of molecules (...
- Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors
[作者:Hamada, S; Kim, TD; Suzuki, T; Itoh, Y; Tsumoto, H; Nakagawa, H; Janknecht, R; Miyata, N,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2852-2855 , 文章类型: Article,,卷期:2009年19-10]
- N-Oxalylglycine (NOG) derivatives were synthesized, and their inhibitory effect on histone lysine demethylase activity was evaluated. NOG and compound 1 inhibited histone lysine demethylases JMJD2A, 2C and 2D in enzyme a...
- Syntheses of low-hemolytic antimicrobial gratisin peptides
[作者:Tamaki, M; Kokuno, M; Sasaki, I; Suzuki, Y; Iwama, M; Saegusa, K; Kikuchi, Y; Shindo, M; Kimura, M; Uchida, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2856-2859 , 文章类型: Article,,卷期:2009年19-10]
- Antibiotic and hemolytic activities of gratisin (GR), cyclo(-Val(1)-Orn(2)-Leu(3)-D-Phe(4)-Pro(5)-D-Tyr(6)-)(2), and. fifteen GR analogues, which have various D-amino acid residues in place of D-Tyr(6,6') residues, were ...
- Discovery of 5-substituted 2-amino-4-chloro-8-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7,8-dihydropteridin-6(5H)-ones as potent and selective Hsp90 inhibitors
[作者:Li, XY; Shocron, E; Song, AM; Patel, N; Sun, CL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2860-2864 , 文章类型: Article,,卷期:2009年19-10]
- A new series of compounds, 5-substituted 2-amino-4-chloro-8-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7,8-dihydropteridin-6(5H)-ones, have been designed and identified as potent and selective inhibitors of Hsp90. Thes...
- Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH)
[作者:Johnson, DS; Ahn, K; Kesten, S; Lazerwith, SE; Song, Y; Morris, M; Fay, L; Gregory, T; Stiff, C; Dunbar, JB; Liimatta, M; Beidler, D; Smith, S; Nomanbhoy, TK; Cravatt, BF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2865-2869 , 文章类型: Article,,卷期:2009年19-10]
- The synthesis and structure-activity relationships (SAR) of a series of benzothiophene piperazine and piperidine urea FAAH inhibitors is described. These compounds inhibit FAAH by covalently modifying the enzyme's active...
- A new psoralen derivative with enlarged antiproliferative properties
[作者:Via, LD; Gonzalez-Gomez, JC; Perez-Montoto, LG; Santana, L; Uriarte, E; Magno, SM; Gia, O,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2874-2876 , 文章类型: Article,,卷期:2009年19-10]
- Following our results with benzopsoralens as potent photochemotherapeutic agents, we report the antiproliferative evaluation of nitrogenated isoster upon and without UVA irradiation. The evaluated pyridazinopsoralen show...
- Enhanced activity or resistance of adenosine derivatives towards adenosine deaminase-catalyzed deamination: Influence of ribose modifications
[作者:Vistoli, G; Pedretti, A; Alessandrini, L; Casati, S; Ciuffreda, P; Meroni, G; Santaniello, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2877-2879 , 文章类型: Article,,卷期:2009年19-10]
- The effect of the presence of the 1'-C-methyl group and 2',3'-O-substitution in the adenosine structure on ADA activity has been investigated by modeling studies. Results show that the 2'- and 3'-O-substituents are harbo...
- Synthesis and bioactivity of a side chain bridged paclitaxel: A test of the T-Taxol conformation
[作者:Hodge, M; Chen, QH; Bane, S; Sharma, S; Loew, M; Banerjee, A; Alcaraz, AA; Snyder, JP; Kingston, DGI,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2884-2887 , 文章类型: Article,,卷期:2009年19-10]
- A knowledge of the bioactive tubulin-binding conformation of paclitaxel (Taxol(TM)) is crucial to a full understanding of the bioactivity of this important anticancer drug, and potentially also to the design of simplifie...
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