- Identification of non-lipid LPA3 antagonists by virtual screening.
[作者:Fells, James I.;Tsukahara, Ryoko;Fujiwara, Yuko;Liu, Jianxiong;Perygin, Donna H.;Osborne, Daniel A.;Tigyi, Gabor;Parrill, Abby L.;,期刊:Bioorganic & Medicinal Chemistry, 页码:6207-6217 , 文章类型: 研究论文,,卷期:2008年16-11]
- In the present study, the authors utilized virtual screening to identify LPA3 antagonists. The authors have developed a three-point structure-based pharmacophore model based on known LPA3 antagonists. This model was us...
- Synthesis, fluorine-18 radiolabeling, and in vitro characterization of 1-iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinolinecarboxamide derivatives as potential PET radioligands for imaging peripheral benzodiazepine receptor.
[作者:Yu, Weiping;Wang, Eric;Voll, Ronald J.;Miller, Andrew H.;Goodman, Mark M.;,期刊:Bioorganic & Medicinal Chemistry, 页码:6145-6155 , 文章类型: 研究论文,,卷期:2008年16-11]
- 1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxa mide (PK11195) has been shown to bind strongly and selectively to the peripheral benzodiazepine receptor (PBR) binding sites. A series of PK11195 anal...
- Synthesis, induced-fit docking investigations, and in vitro aldose reductase inhibitory activity of non-carboxylic acid containing 2,4-thiazolidinedione derivatives.
[作者:Maccari, Rosanna;Ottana, Rosaria;Ciurleo, Rosella;Rakowitz, Dietmar;Matuszczak, Barbara;Laggner, Christian;Langer, Thierry;,期刊:Bioorganic & Medicinal Chemistry, 页码:5840-5852 , 文章类型: 研究论文,,卷期:2008年16-11]
- In continuation of our studies, we here report a series of non-carboxylic acid contg. 2,4-thiazolidinedione derivs., analogs of previously synthesized carboxylic acids which we had found to be very active in vitro aldose...
- Anti-Helicobacter pylori activity of derivatives of the phthalide-containing antibacterial agents spirolaxine methyl ether, CJ-12,954, CJ-13,013, CJ-13,102, CJ-13,104, CJ-13,108 and CJ-13,015.
[作者:Radcliff, Fiona J.;Fraser, John D.;Wilson, Zoe E.;Heapy, Amanda M.;Robinson, James E.;Bryant, Christina J.;Flowers, Christopher L.;Brimble, Margaret A.;,期刊:Bioorganic & Medicinal Chemistry, 页码:6179-6185 , 文章类型: 研究论文,,卷期:2008年16-11]
- ether, CJ-12,954, CJ-13,013, CJ-13,015, CJ-13,102, CJ-13,103, CJ-13,104 and CJ-13,108, have been reported to exhibit anti-H. pylori activity. However, the exact stereochem. of spirolaxine Me ether, CJ-12,954 or CJ-13,01...
- E,E-2-Benzylidene-6-(nitrobenzylidene)cyclohexanones: Syntheses, cytotoxicity and an examination of some of their electronic, steric, and hydrophobic properties.
[作者:Das, Umashankar;Doroudi, Alireza;Das, Swagatika;Bandy, Brian;Balzarini, Jan;De Clercq, Erik;Dimmock, Jonathan R.;,期刊:Bioorganic & Medicinal Chemistry, 页码:6261-6268 , 文章类型: 研究论文,,卷期:2008年16-11]
- Three series of structurally isomeric 2-benzylidene-6-(nitrobenzylidene) cyclohexanones 1-3 were prepd. and evaluated against human Molt/C8 and CEM T-lymphocytes as well as murine L1210 cells. The IC50 values of the maj...
- Structure and bioactivity of the polysaccharides in medicinal plant Dendrobium huoshanense.
[作者:Hsieh, Yves S.-Y.;Chien, Cheng;Liao, Sylvian K.-S.;Liao, Shih-Fen;Hung, Wei-Ting;Yang, Wen-Bin;Lin, Chih-Chien;Cheng, Ting-Jen Rachel;Chang, Chia-Chuan;Fang, Jim-Min;Wong, Chi-Huey;,期刊:Bioorganic & Medicinal Chemistry, 页码:6054-6068 , 文章类型: 研究论文,,卷期:2008年16-11]
- Detailed structures of the active polysaccharides extd. from the leaf and stem cell walls and mucilage of Dendrobium huoshanense are detd. by using various techniques, including chromatog., spectroscopic, chem., and enzy...
- Pestaloficiols A-E, bioactive cyclopropane derivatives from the plant endophytic fungus Pestalotiopsis fici.
[作者:Liu, Ling;Tian, Renrong;Liu, Shuchun;Chen, Xulin;Guo, Liangdong;Che, Yongsheng;,期刊:Bioorganic & Medicinal Chemistry, 页码:6021-6026 , 文章类型: 研究论文,,卷期:2008年16-11]
- Pestaloficiols A-E (1-5), five new cyclopropane derivs., have been isolated from cultures of the plant endophyte Pestalotiopsis fici. The structures of these compds. were detd. by NMR spectroscopy, and the abs. configur...
- Selection of phage-displayed peptides that bind to a particular ligand-bound antibody.
[作者:Tanaka, Fujie;Hu, Yunfeng;Sutton, Jori;Asawapornmongkol, Lily;Fuller, Roberta;Olson, Arthur J.;Barbas, Carlos F., III;Lerner, Richard A.;,期刊:Bioorganic & Medicinal Chemistry, 页码:5926-5931 , 文章类型: 研究论文,,卷期:2008年16-11]
- Phage-displayed peptides that selectively bind to aldolase catalytic antibody 93F3 when bound to a particular 1,3-diketone hapten deriv. have been developed using designed selection strategies with libraries contg. 7-12 ...
- Synthesis, nano-scale assembly, and in vivo anti-thrombotic activity of novel short peptides containing L-Arg and L-Asp or L-Glu.
[作者:Chen, Yu;Cui, Guohui;Zhao, Ming;Wang, Chao;Qian, Keduo;Morris-Natschke, Susan;Lee, Kuo-Hsiung;Peng, Shiqi;,期刊:Bioorganic & Medicinal Chemistry, 页码:5914-5925 , 文章类型: 研究论文,,卷期:2008年16-11]
- Two tripeptides H-Asp(Arg)-Arg (3a) and H-Glu(Arg)-Arg (3b), four pentapeptides H-Asp(Arg-Asp)-Arg-Asp (6a), H-Glu(Arg-Asp)-Arg-Asp (6b), H-Asp(Asp-Arg)-Asp-Arg (10a), and H-Glu(Asp-Arg)-Asp-Arg (10b), and their Cu(II)-p...
- High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): A high-affinity 5-HT2A receptor-selective agonist radioligand.
[作者:Nichols, David E.;Frescas, Stewart P.;Chemel, Benjamin R.;Rehder, Kenneth S.;Zhong, Desong;Lewin, Anita H.;,期刊:Bioorganic & Medicinal Chemistry, 页码:6116-6123 , 文章类型: 研究论文,,卷期:2008年16-11]
- The title compd. ([3H]INBMeO) was prepd. by an O,O-dimethylation reaction of a t-BOC protected diphenolic precursor using no carrier added tritiated iodomethane in DMF with K2CO3. Removal of the t-BOC protecting group a...
- Design of antiangiogenic hypoxic cell radiosensitizers: 2-Nitroimidazoles containing a 2-aminomethylene-4-cyclopentene-1,3-dione moiety.
[作者:Uto, Yoshihiro;Nagasawa, Hideko;Jin, Cheng-Zhe;Nakayama, Shinichi;Tanaka, Ayako;Kiyoi, Saori;Nakashima, Hitomi;Shimamura, Mariko;Inayama, Seiichi;Fujiwara, Tomoya;Takeuchi, Yoshio;Uehara, Yoshimasa;Kirk, Kenneth L.;Nakata, Eiji;Hori, Hitoshi;,期刊:Bioorganic & Medicinal Chemistry, 页码:6042-6053 , 文章类型: 研究论文,,卷期:2008年16-11]
- We designed chiral 2-nitroimidazole derivs. contg. a 2-aminomethylene-4-cyclopentene-1,3-dione moiety as antiangiogenic hypoxic cell radiosensitizers. Based on results of MO calcns., the 2-aminomethylene-4-cyclopentene-...
- Analogs of Eu3+ DOTAM-Gly-Phe-OH and Tm3+ DOTAM-Gly-Lys-OH: Synthesis and magnetic properties of potential PARACEST MRI contrast agents.
[作者:Suchy, Mojmir;Li, Alex X.;Bartha, Robert;Hudson, Robert H. E.;,期刊:Bioorganic & Medicinal Chemistry, 页码:6156-6166 , 文章类型: 研究论文,,卷期:2008年16-11]
- Chelated lanthanide ions, esp. gadolinium, have found wide use as contrast agents in magnetic resonance imaging. A new paradigm for generating contrast, termed PARACEST, was recently described that requires the slow exc...
- Genotoxicity of a-asarone analogues.
[作者:Karwicka, Ewa;Marczewska, Jadwiga;Anuszewska, Elzbieta;Lozowicka, Bozena;Chilmonczyk, Zdzislaw;,期刊:Bioorganic & Medicinal Chemistry, 页码:6069-6074 , 文章类型: 研究论文,,卷期:2008年16-11]
- The role of cholesterol in the formation of atherosclerotic lesions during hypercholesterolemia has been confirmed. a-Asarone is a substance of a potent hypolipidemic activity which is isolated from plants. We previous...
- Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
[作者:Koda, Yasuko;Del Borgo, Mark;Wessling, Susanne T.;Lazarus, Lawrence H.;Okada, Yoshio;Toth, Istvan;Blanchfield, Joanne T.;,期刊:Bioorganic & Medicinal Chemistry, 页码:6286-6296 , 文章类型: 研究论文,,卷期:2008年16-11]
- Endomorphin 1 (Endo-1 = Tyr-Pro-Trp-Phe-NH2), an endogenous opioid with high affinity and selectivity for m-opioid receptors, mediates acute and neuropathic pain in rodents. To overcome metabolic instability and poor me...
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