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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共23条记录   Docking study, synthesis, and in vitro evaluation of fluoro-MADAM derivatives as SERT ligands for PET imaging. [作者：Mavel, Sylvie;Vercouillie, Johnny;Garreau, Lucette;Raguza, Tiziana;Ravna, Aina Westrheim;Chalon, Sylvie;Guilloteau, Denis;Emond, Patrick;,期刊：Bioorganic & Medicinal Chemistry, 页码：9050-9055 , 文章类型： 研究论文，,卷期：2008年16-19] In order to predict affinity of new diphenylsulfides for the serotonin transporter (SERT), a mol. modeling model was used to compare potential binding affinity of new compds. with known potent ligands. The aim of this st... Deuterium isotope effects for the oxidation of 1-methyl-3-phenyl-3-pyrrolinyl analogues by monoamine oxidase B. [作者：Pretorius, Anel;Ogunrombi, Modupe O.;Terre'Blanche, Gisella;Castagnoli, Neal, Jr.;Bergh, Jacobus J.;Petzer, Jacobus P.;,期刊：Bioorganic & Medicinal Chemistry, 页码：8813-8817 , 文章类型： 研究论文，,卷期：2008年16-19] The parkinsonian inducing agent, 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), is a cyclic tertiary allylamine exhibiting good monoamine oxidase B (MAO-B) substrate properties. MAO-B catalyzes the ring a-carbon 2... Structure-activity study at positions 3 and 4 of human neuropeptide S. [作者：Camarda, Valeria;Trapella, Claudio;Calo', Girolamo;Guerrini, Remo;Rizzi, Anna;Ruzza, Chiara;Fiorini, Stella;Marzola, Erika;Reinscheid, Rainer K.;Regoli, Domenico;Salvadori, Severo;,期刊：Bioorganic & Medicinal Chemistry, 页码：8841-8845 , 文章类型： 研究论文，,卷期：2008年16-19] Neuropeptide S (NPS) has been identified as the endogenous ligand of a previously orphan receptor now named NPSR. Previous studies demonstrated that the N-terminal sequence Phe2-Arg3-Asn4 of the peptide is crucial for b... Specific targeting of metzincin family members with small-molecule inhibitors: Progress toward a multifarious challenge. [作者：Georgiadis, Dimitris;Yiotakis, Athanasios;,期刊：Bioorganic & Medicinal Chemistry, 页码：8781-8794 , 文章类型： 综述，,卷期：2008年16-19] A review. Zn-metalloproteinases are an important class of hydrolytic atom in their active center which is fundamental for proteolytic activity. Metzincins, a superfamily of Zn-metalloproteinases with many structural and... Fluorescent polycyclic ligands for nitric oxide synthase (NOS) inhibition. [作者：Joubert, Jacques;van Dyk, Sandra;Malan, Sarel F.;,期刊：Bioorganic & Medicinal Chemistry, 页码：8952-8958 , 文章类型： 研究论文，,卷期：2008年16-19] In recent years polycyclic compds. have been shown to exhibit pharmacol. profiles of importance in the symptomatic and proposed curative treatment of neurodegenerative diseases (e.g., Parkinson's and Alzheimer's disease)... Antioxidative and thrombolytic TMP nitrone for treatment of ischemic stroke. [作者：Sun, Yewei;Jiang, Jie;Zhang, Zaijun;Yu, Pei;Wang, Linda;Xu, Changlin;Liu, Wei;Wang, Yuqiang;,期刊：Bioorganic & Medicinal Chemistry, 页码：8868-8874 , 文章类型： 研究论文，,卷期：2008年16-19] Ischemic stroke results from brain blood vessel blockage by thrombus, and produces neuronal cell damage and death. While thrombolytic therapy with tPA has achieved some success in clinic, the strategy of using neuroprot... Development of a second generation of inhibitors of microsomal prostaglandin E synthase 1 expression bearing the g-hydroxybutenolide scaffold. [作者：Aquino, Maurizio;Guerrero, Maria D.;Bruno, Ines;Terencio, Maria C.;Paya, Miguel;Riccio, Raffaele;,期刊：Bioorganic & Medicinal Chemistry, 页码：9056-9064 , 文章类型： 研究论文，,卷期：2008年16-19] Petrosaspongiolide M (PM) a marine sesterterpene metabolite bearing the g-hydroxybutenolide scaffold and displaying a potent inhibitory activity toward PLA2 enzyme, was selected by the authors as an attractive target to ... RCAI-17, 22, 24-26, 29, 31, 34-36, 38-40, and 88, the analogs of KRN7000 with a sulfonamide linkage: Their synthesis and bioactivity for mouse natural killer T cells to produce Th2-biased cytokines. [作者：Tashiro, Takuya;Hongo, Naomi;Nakagawa, Ryusuke;Seino, Ken-ichiro;Watarai, Hiroshi;Ishii, Yasuyuki;Taniguchi, Masaru;Mori, Kenji;,期刊：Bioorganic & Medicinal Chemistry, 页码：8896-8906 , 文章类型： 研究论文，,卷期：2008年16-19] KRN7000 with a sulfonamide linkage instead of an amide bond, were synthesized to examine their bioactivity for mouse natural killer (NK) T cells. RCAI-17, 22, 24-26, 29, 31, 34-36, and 88 are the arom. sulfonamide analo... Peptidyl epoxides extended in the P' direction as cysteine protease inhibitors: Effect on affinity and mechanism of inhibition. [作者：Perlman, Nurit;Hazan, Maya;Shokhen, Michael;Albeck, Amnon;,期刊：Bioorganic & Medicinal Chemistry, 页码：9032-9039 , 文章类型： 研究论文，,卷期：2008年16-19] the scissile amide bond of a P3-P3' peptide, were designed as cysteine proteases inhibitors. The addnl. P'-S' interactions, relative to those of an exo peptidyl epoxide of the same P3-P1 sequence, significantly improved... Synthesis and antituberculosis activity of 5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazone derivatives. [作者：Guzel, Ozlen;Karali, Nilgun;Salman, Aydin;,期刊：Bioorganic & Medicinal Chemistry, 页码：8976-8987 , 文章类型： 研究论文，,卷期：2008年16-19] New series of 5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazones, 1-methyl-5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazones and 5-trifluoromethoxy-1-morpholinomethyl-1H-indole-2,3-dione ... Synthesis and immunological evaluation of self-adjuvanting glycolipopeptide vaccine candidates. [作者：Fujita, Yoshio;Abdel-Aal, Abu-Baker M.;Wimmer, Norbert;Batzloff, Michael R.;Good, Michael F.;Toth, Istvan;,期刊：Bioorganic & Medicinal Chemistry, 页码：8907-8913 , 文章类型： 研究论文，,卷期：2008年16-19] Synthesis of four glycolipids with different no. of lauroyl groups on glucose or cellobiose as scaffolds is described. Their immunol. evaluations either admixed with or covalently linked to J8, a peptide antigen derived... Synthesis and anticonvulsant activities of N-benzyl (2R)-2-acetamido-3-oxysubstituted propionamide derivatives. [作者：Morieux, Pierre;Stables, James P.;Kohn, Harold;,期刊：Bioorganic & Medicinal Chemistry, 页码：8968-8975 , 文章类型： 研究论文，,卷期：2008年16-19] Lacosamide has been submitted for regulatory approval in the United States and Europe for the treatment of epilepsy. Previous synthetic methods did not permit the elaboration of the structure-activity relationship (SAR)... Bisphosphonate inhibitors of ATP-mediated HIV-1 reverse transcriptase catalyzed excision of chain-terminating 3'-azido, 3'-deoxythymidine: A QSAR investigation. [作者：Song, Yongcheng;Chan, Julian M. W.;Tovian, Zev;Secrest, Aaron;Nagy, Eva;Krysiak, Kilannin;Bergan, Kyle;Parniak, Michael A.;Oldfield, Eric;,期刊：Bioorganic & Medicinal Chemistry, 页码：8959-8967 , 文章类型： 研究论文，,卷期：2008年16-19] ATP-mediated HIV-1 reverse transcriptase catalyzed phosphorolysis in vitro of AZT from AZT-terminated DNA primers by a series of 42 bisphosphonates. The four most active compds. possess neutral, halogen-substituted Ph o... New potent cathepsin G phosphonate inhibitors. [作者：Sienczyk, Marcin;Lesner, Adam;Wysocka, Magdalena;Legowska, Anna;Pietrusewicz, Ewa;Rolka, Krzysztof;Oleksyszyn, Jozef;,期刊：Bioorganic & Medicinal Chemistry, 页码：8863-8867 , 文章类型： 研究论文，,卷期：2008年16-19] Cathepsin G is an enzyme with dual chymotrypsin and trypsin-like specificity. As a leukocyte proteinase it is involved in the early stages of the immune response. In this work the synthesis and inhibitory activity of d... Synthesis and biological evaluation of polymethoxylated 4-heteroarylcoumarins as tubulin assembly inhibitor. [作者：Ganina, Olga G.;Daras, Etienne;Bourgarel-Rey, Veronique;Peyrot, Vincent;Andresyuk, Alexey N.;Finet, Jean-Pierre;Fedorov, Alexey Yu.;Beletskaya, Irina P.;Combes, Sebastien;,期刊：Bioorganic & Medicinal Chemistry, 页码：8806-8812 , 文章类型： 研究论文，,卷期：2008年16-19] A series of syn-restricted polymethoxylated 4-heteroarylcoumarins-the isostructural analogs of combretastatin A-4-was synthesized by Suzuki-Miyaura cross-coupling reaction and evaluated for antiproliferative activity. T... Insights into the mechanism of Na+,K+-ATPase inhibition by 2-methoxy-3,8,9-trihydroxy coumestan. [作者：Pocas, Elisa S. C.;Touza, Natalia A.;Pimenta, Paulo H. C.;Leitao, Fernanda B.;Neto, Chaquip D.;da Silva, Alcides J. M.;Costa, Paulo R. R.;Noel, Francois;,期刊：Bioorganic & Medicinal Chemistry, 页码：8801-8805 , 文章类型： 研究论文，,卷期：2008年16-19] The mol. mechanisms involved in Na+,K+-ATPase inhibition by 2-methoxy-3,8,9-trihydroxy coumestan were investigated. The authors show that this compd. decreases the free sulfydryl groups present in the enzyme and that it...