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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33条记录   Genome mining for novel natural product discovery. [作者：Challis, Gregory L.;,期刊：Journal of Medicinal Chemistry, 页码：2618-2628 , 文章类型： 综述，,卷期：2008年51-9] A review. The future of genome mining for new natural product discovery seems bright and it is likely that the coming years will see an explosion of interest in this exciting field. Genomic mining approaches are likely... Modern Natural Products Chemistry and Drug Discovery. [作者：Ojima, Iwao;,期刊：Journal of Medicinal Chemistry, 页码：2587-2588 , 文章类型： 综述，,卷期：2008年51-9] A review. Natural products chem. has provided impressive "chem. diversity space". The secondary metabolites of diverse life forms have potent biol. activities and have provided lead compds. in drug discovery for the tr... Novel Potent and Selective Thrombin Inhibitors Based on a Central 1,4-Benzoxazin-3(4H)-one Scaffold. [作者：Ilas, Janez;Tomas, Tihomir;Kikelj, Danijel;,期刊：Journal of Medicinal Chemistry, 页码：2863-2867 , 文章类型： 研究论文，,卷期：2008年51-9] scaffold, benzamidine P1 arginine side chain mimetic and various P3 moieties are described. The most potent compd. (I) in the series, exhibited a Ki of 2.6 nM in vitro for thrombin and high selectivity against trypsin a... Aza-peptidyl Michael Acceptors. A New Class of Potent and Selective Inhibitors of Asparaginyl Endopeptidases (Legumains) from Evolutionarily Diverse Pathogens. [作者：Goetz, Marion G.;Ellis James, Karen;Hansell, Elizabeth;Dvorak, Jan;Seshaadri, Amritha;Sojka, Daniel;Kopacek, Petr;McKerrow, James H.;Caffrey, Conor R.;Powers, James C.;,期刊：Journal of Medicinal Chemistry, 页码：2816-2832 , 文章类型： 研究论文，,卷期：2008年51-9] Aza-peptide Michael acceptors with the general structure of Cbz-Ala-Ala-NHN(CH2CONH2)COCH=CHCONR1R2 [NR1R2 = NEt2, NBu2, piperidine, NHPh, NHCH2Ph, NHCH2CH2Ph, N(Me)Ph, N(Me)CH2Ph, N(Me)CH2-1-naphthyl, N(Me)CH2CH2Ph, N(C... Design and Synthesis of Conformationally Constrained Glucagon-Like Peptide-1 Derivatives with Increased Plasma Stability and Prolonged in Vivo Activity. [作者：Miranda, Les P.;Winters, Katherine A.;Gegg, Colin V.;Patel, Ankita;Aral, Jennifer;Long, Jason;Zhang, Jingwen;Diamond, Stephanie;Guido, Mark;Stanislaus, Shanaka;Ma, Mark;Li, Hongyan;Rose, Mark J.;Poppe, Leszek;Veniant, Murielle M.;,期刊：Journal of Medicinal Chemistry, 页码：2758-2765 , 文章类型： 研究论文，,卷期：2008年51-9] A series of conformationally constrained derivs. of glucagon-like peptide-1 (GLP-1) were designed and evaluated. By use of [Gly8]GLP-1(7-37)-NH2 (2) peptide as a starting point, 17 cyclic derivs. possessing i to i + 4, ... Design and Microwave-Assisted Synthesis of Novel Macrocyclic Peptides Active at Melanocortin Receptors: Discovery of Potent and Selective hMC5R Receptor Antagonists. [作者：Grieco, Paolo;Cai, Minying;Liu, Lu;Mayorov, Alexander;Chandler, Kevin;Trivedi, Dev;Lin, Guangxin;Campiglia, Pietro;Novellino, Ettore;Hruby, Victor J.;,期刊：Journal of Medicinal Chemistry, 页码：2701-2707 , 文章类型： 研究论文，,卷期：2008年51-9] Differentiation of the physiol. role of the melanocortin receptor 5 MC5R from that of other melanocortin receptors will require development of high affinity and selective antagonists. To date, a few synthetic antagonist... Ring Size in Octreotide Amide Modulates Differently Agonist versus Antagonist Binding Affinity and Selectivity. [作者：Grace, Christy Rani R.;Erchegyi, Judit;Samant, Manoj;Cescato, Renzo;Piccand, Veronique;Riek, Roland;Reubi, Jean Claude;Rivier, Jean E.;,期刊：Journal of Medicinal Chemistry, 页码：2676-2681 , 文章类型： 研究论文，,卷期：2008年51-9] H-DPhe2-c[Cys3-Phe7-DTrp8-Lys9-Thr10-Cys14]-Thr15-NH2 (1) (a somatostatin agonist, SRIF numbering) and H-Cpa2-c[DCys3-Tyr7-DTrp8-Lys9-Thr10-Cys14]-Nal15-NH2 (4) (a somatostatin antagonist) are based on the structure of o... Ring Size of Somatostatin Analogues (ODT-8) Modulates Receptor Selectivity and Binding Affinity. [作者：Erchegyi, Judit;Grace, Christy Rani R.;Samant, Manoj;Cescato, Renzo;Piccand, Veronique;Riek, Roland;Reubi, Jean Claude;Rivier, Jean E.;,期刊：Journal of Medicinal Chemistry, 页码：2668-2675 , 文章类型： 研究论文，,卷期：2008年51-9] The synthesis, biol. testing, and NMR studies of several analogs of H-cyclo[Cys3-Phe6-Phe7-D-Trp8-Lys9-Thr10-Phe11-Cys14]-OH (ODT-8, a pan-somatostatin analog, 1) have been performed to assess the effect of changing the ... Degradation of Bidentate-Coordinated Platinum(II)-Based DNA Intercalators by Reduced L-Glutathione. [作者：Kemp, Sharon;Wheate, Nial J.;Pisani, Michelle J.;Aldrich-Wright, Janice R.;,期刊：Journal of Medicinal Chemistry, 页码：2787-2794 , 文章类型： 研究论文，,卷期：2008年51-9] We have examd. the interaction of [(5,6-dimethyl-1,10-phenanthroline)(1S,2S-diaminocyclohexane)platinu m(II)]2+ (56MESS), ]2+(5MESS), [(5,6-dimethyl-1,10-phenanthroline)(1R,2R-diaminocyclohexane)platinu m(II)]2+ (56MERR)... Synthesis and screening of mono- and di-aryl technetium and rhenium metallocarboranes. A new class of probes for the estrogen receptor. [作者：Causey, Patrick W.;Besanger, Travis R.;Valliant, John F.;,期刊：Journal of Medicinal Chemistry, 页码：2833-2844 , 文章类型： 研究论文，,卷期：2008年51-9] (Organometallic and Organometalloidal Compounds) Section A series of mono- and diaryl-substituted rhenium(I) closo-2,1,8-rhenacarboranes were prepd. by microwave-assisted reaction of closo-carborane with [Re(CO)3(H2O)3]B... Design and Synthesis of 2- and 3-Substituted-3-phenylpropyl Analogs of 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: Role of Amino, Fluoro, Hydroxyl, Methoxyl, Methyl, M [作者：Hsin, Ling-Wei;Chang, Li-Te;Rothman, Richard B.;Dersch, Christina M.;Jacobson, Arthur E.;Rice, Kenner C.;,期刊：Journal of Medicinal Chemistry, 页码：2795-2806 , 文章类型： 研究论文，,卷期：2008年51-9] (Heterocyclic Compounds (More Than One Hetero Atom)) Section Novel derivs. of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) and with various substituents in positions C2 and C3 of the p... Synthesis and Pharmacological Evaluations of Sildenafil Analogues for Treatment of Erectile Dysfunction. [作者：Flores Toque, Haroldo A.;Priviero, Fernanda B. M.;Teixeira, Cleber E.;Perissutti, Elisa;Fiorino, Ferdinando;Severino, Beatrice;Frecentese, Francesco;Lorenzetti, Raquel;Baracat, Juliana S.;Santagada, Vincenzo;Caliendo, Giuseppe;Antunes, Edson;De Nucci, Gil,期刊：Journal of Medicinal Chemistry, 页码：2807-2815 , 文章类型： 研究论文，,卷期：2008年51-9] The 5-[2-ethoxy-5-(4-methylpiperazin-1-ylsulfonyl)phenyl]-1-methyl-3-propyl- 1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one, sildenafil, is a cGMP-specific phosphodiesterase-5 (PDE5) inhibitor used for penile erectile dys... Synthesis and Structure-Activity Relationships of 4-Pyridones as Potential Antimalarials. [作者：Yeates, Clive L.;Batchelor, John F.;Capon, Edward C.;Cheesman, Neil J.;Fry, Mitch;Hudson, Alan T.;Pudney, Mary;Trimming, Helen;Woolven, James;Bueno, Jose M.;Chicharro, Jesus;Fernandez, Esther;Fiandor, Jose M.;Gargallo-Viola, Domingo;Gomez de las Heras, Fe,期刊：Journal of Medicinal Chemistry, 页码：2845-2852 , 文章类型： 研究论文，,卷期：2008年51-9] A series of diaryl ether substituted 4-pyridones, e.g. I (R1 = H, Br, Cl, OMe, NO2, etc.; R2 = Ph, 4-FC6H4, 3-F3CC6H4, 4-F3COC6H4, etc.), have been identified as having potent antimalarial activity superior to that of ch... Combining Docking, Molecular Dynamics and the Linear Interaction Energy Method to Predict Binding Modes and Affinities for Non-nucleoside Inhibitors to HIV-1 Reverse Transcriptase. [作者：Carlsson, Jens;Boukharta, Lars;Aqvist, Johan;,期刊：Journal of Medicinal Chemistry, 页码：2648-2656 , 文章类型： 研究论文，,卷期：2008年51-9] energy (LIE) method are used here to predict binding modes and affinities for a set of 43 non-nucleoside inhibitors to HIV-1 reverse transcriptase. Starting from a crystallog. structure, the binding modes of 43 inhibito... Predicting Binding Modes from Free Energy Calculations. [作者：Nervall, Martin;Hanspers, Peter;Carlsson, Jens;Boukharta, Lars;Aqvist, Johan;,期刊：Journal of Medicinal Chemistry, 页码：2657-2667 , 文章类型： 研究论文，,卷期：2008年51-9] challenge in the field of structure-based inhibitor design and is a requirement for accurate binding free energy predictions with structure-based methods. A series of HIV-1 reverse transcriptase inhibitors was cross-doc... Identification of Plasmodium falciparum Spermidine Synthase Active Site Binders through Structure-Based Virtual Screening. [作者：Jacobsson, Micael;Garedal, Magnus;Schultz, Johan;Karlen, Anders;,期刊：Journal of Medicinal Chemistry, 页码：2777-2786 , 文章类型： 研究论文，,卷期：2008年51-9] falciparum spermidine synthase, were identified by structure-based virtual screening. The binding of these compds. was exptl. verified by NMR techniques. Spermidine synthase, an enzyme involved in the polyamine pathway...