- 4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H -phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1.
[作者:Menear, Keith A.;Adcock, Claire;Boulter, Robert;Cockcroft, Xiao-ling;Copsey, Louise;Cranston, Aaron;Dillon, Krystyna J.;Drzewiecki, Jan;Garman, Sheila;Gomez, Sylvie;Javaid, Hashim;Kerrigan, Frank;Knights, Charlotte;Lau, Alan;Loh, Vincent M., Jr.;Matthews,,期刊:Journal of Medicinal Chemistry, 页码:6581-6591 , 文章类型: 研究论文,,卷期:2008年51-20]
- Poly(ADP-ribose) polymerase activation is an immediate cellular response to metabolic-, chem.-, or ionizing radiation-induced DNA damage and represents a new target for cancer therapy. In this article, we disclose a nov...
- Structure-Activity Relationships in 1,4-Benzodioxan-Related Compounds. 9. From 1,4-Benzodioxane to 1,4-Dioxane Ring as a Promising Template of Novel a1D-Adrenoreceptor Antagonists, 5-HT1A Full Agonists, and Cytotoxic Agents.
[作者:Quaglia, Wilma;Piergentili, Alessandro;Del Bello, Fabio;Farande, Yogita;Giannella, Mario;Pigini, Maria;Rafaiani, Giovanni;Carrieri, Antonio;Amantini, Consuelo;Lucciarini, Roberta;Santoni, Giorgio;Poggesi, Elena;Leonardi, Amedeo;,期刊:Journal of Medicinal Chemistry, 页码:6359-6370 , 文章类型: 研究论文,,卷期:2008年51-20]
- Novel 1,4-dioxane compds. structurally related to WB 4101 (I) were prepd. in order to investigate the possibility that the quite planar 1,4-benzodioxane template of I might be replaced by the less conformationally constr...
- Synthesis and Structure-Activity Relationship Studies of Highly Potent Novel Oxazolidinone Antibacterials.
[作者:Komine, Takashi;Kojima, Akihiko;Asahina, Yoshikazu;Saito, Tatsuhiro;Takano, Hisashi;Shibue, Taku;Fukuda, Yasumichi;,期刊:Journal of Medicinal Chemistry, 页码:6558-6562 , 文章类型: 研究论文,,卷期:2008年51-20]
- Novel antibacterial biaryl oxazolidinones, e.g. I, bearing an aza-, an oxa-, or a thiabicyclo[3.1.0]hex-6-yl ring system were synthesized, and their in vitro antibacterial activity and structure-activity relationships (S...
- Modified Peptides as Potent Inhibitors of the Postsynaptic Density-95/N-Methyl-D-Aspartate Receptor Interaction.
[作者:Bach, Anders;Chi, Celestine N.;Olsen, Thomas B.;Pedersen, Soren W.;Roder, Martin U.;Pang, Gar F.;Clausen, Rasmus P.;Jemth, Per;Stromgaard, Kristian;,期刊:Journal of Medicinal Chemistry, 页码:6450-6459 , 文章类型: 研究论文,,卷期:2008年51-20]
- The protein-protein interaction between the NMDA receptor and its intracellular scaffolding protein, PSD-95, is a potential target for treatment of ischemic brain diseases. An undecapeptide corresponding to the C-termin...
- Modeling Binding Modes of a7 Nicotinic Acetylcholine Receptor with Ligands: The Roles of Gln117 and Other Residues of the Receptor in Agonist Binding.
[作者:Huang, Xiaoqin;Zheng, Fang;Stokes, Clare;Papke, Roger L.;Zhan, Chang-Guo;,期刊:Journal of Medicinal Chemistry, 页码:6293-6302 , 文章类型: 研究论文,,卷期:2008年51-20]
- Extensive mol. docking, mol. dynamics simulations, and binding free energy calcns. have been performed to understand how a7-specific agonists of nicotinic acetylcholine receptor (nAChR), including AR-R17779 (1), GTS-21 (...
- The Importance of Micelle-Bound States for the Bioactivities of Bifunctional Peptide Derivatives for d/m Opioid Receptor Agonists and Neurokinin 1 Receptor Antagonists.
[作者:Yamamoto, Takashi;Nair, Padma;Jacobsen, Neil E.;Davis, Peg;Ma, Shou-wu;Navratilova, Edita;Moye, Sharif;Lai, Josephine;Yamamura, Henry I.;Vanderah, Todd W.;Porreca, Frank;Hruby, Victor J.;,期刊:Journal of Medicinal Chemistry, 页码:6334-6347 , 文章类型: 研究论文,,卷期:2008年51-20]
- To provide new insight into the detg. factors of membrane-bound peptide conformation that might play an important role in peptide-receptor docking and further biol. behaviors, the dodecylphosphocholine (DPC) micelle-boun...
- A Copper(I)-Catalyzed 1,2,3-Triazole Azide-Alkyne Click Compound Is a Potent Inhibitor of a Multidrug-Resistant HIV-1 Protease Variant.
[作者:Giffin, Michael J.;Heaslet, Holly;Brik, Ashraf;Lin, Ying-Chuan;Cauvi, Gabrielle;Wong, Chi-Huey;McRee, Duncan E.;Elder, John H.;Stout, C. David;Torbett, Bruce E.;,期刊:Journal of Medicinal Chemistry, 页码:6263-6270 , 文章类型: 研究论文,,卷期:2008年51-20]
- Treatment with HIV-1 protease inhibitors, a component of highly active antiretroviral therapy (HAART), often results in viral resistance. Structural and biochem. characterization of a 6X protease mutant arising from in v...
- Identification of Non-Nucleoside DNA Synthesis Inhibitors of Vaccinia Virus by High-Throughput Screening.
[作者:Ciustea, Mihai;Silverman, Janice Elaine Y.;Druck Shudofsky, Abigail M.;Ricciardi, Robert P.;,期刊:Journal of Medicinal Chemistry, 页码:6563-6570 , 文章类型: 研究论文,,卷期:2008年51-20]
- Variola virus, the causative agent of smallpox, is a potential bioweapon. The development of new antiviral compds. for smallpox prophylaxis and treatment is crit., esp. because the virus can acquire resistance to the dr...
- Discovery of 1,4-Substituted Piperidines as Potent and Selective Inhibitors of T-Type Calcium Channels.
[作者:Yang, Zhi-Qiang;Barrow, James C.;Shipe, William D.;Schlegel, Kelly-Ann S.;Shu, Youheng;Yang, F. Vivien;Lindsley, Craig W.;Rittle, Kenneth E.;Bock, Mark G.;Hartman, George D.;Uebele, Victor N.;Nuss, Cindy E.;Fox, Steve V.;Kraus, Richard L.;Doran, Scott M.;,期刊:Journal of Medicinal Chemistry, 页码:6471-6477 , 文章类型: 研究论文,,卷期:2008年51-20]
- The discovery of a novel series of potent and selective T-type calcium channel antagonists is reported. Initial optimization of high-throughput screening leads afforded a 1,4-substituted piperidine amide 6 with good pot...
- Discovery and X-ray Crystallographic Analysis of a Spiropiperidine Iminohydantoin Inhibitor of b-Secretase.
[作者:Barrow, James C.;Stauffer, Shaun R.;Rittle, Kenneth E.;Ngo, Phung L.;Yang, ZhiQiang;Selnick, Harold G.;Graham, Samuel L.;Munshi, Sanjeev;McGaughey, Georgia B.;Holloway, M. Katharine;Simon, Adam J.;Price, Eric A.;Sankaranarayanan, Sethu;Colussi, Dennis;Tug,期刊:Journal of Medicinal Chemistry, 页码:6259-6262 , 文章类型: 研究论文,,卷期:2008年51-20]
- A high-throughput screen at 100 mM inhibitor concn. for the BACE-1 enzyme revealed a novel spiropiperidine iminohydantoin aspartyl protease inhibitor template. An x-ray cocrystal structure with BACE-1 revealed a novel m...
- 1H-Cyclopentapyrimidine-2,4(1H,3H)-dione-Related Ionotropic Glutamate Receptors Ligands. Structure-Activity Relationships and Identification of Potent and Selective iGluR5 Modulators.
[作者:Butini, Stefania;Pickering, Darryl S.;Morelli, Elena;Sanna Coccone, Salvatore;Trotta, Francesco;De Angelis, Meri;Guarino, Egeria;Fiorini, Isabella;Campiani, Giuseppe;Novellino, Ettore;Schousboe, Arne;Christensen, Jeppe K.;Gemma, Sandra;,期刊:Journal of Medicinal Chemistry, 页码:6614-6618 , 文章类型: 研究论文,,卷期:2008年51-20]
- (S)-CPW399 ((S)-1) is a potent and excitotoxic AMPA receptor partial agonist. Modifying the cyclopentane ring of (S)-1, we developed two of the most potent and selective functional antagonists (5 and 7) for kainate rece...
- Combining Ligand-Based Pharmacophore Modeling, Quantitative Structure-Activity Relationship Analysis and in Silico Screening for the Discovery of New Potent Hormone Sensitive Lipase Inhibitors.
[作者:Taha, Mutasem O.;Dahabiyeh, Lina A.;Bustanji, Yasser;Zalloum, Hiba;Saleh, Suhair;,期刊:Journal of Medicinal Chemistry, 页码:6478-6494 , 文章类型: 研究论文,,卷期:2008年51-20]
- Hormone sensitive lipase (HSL) has been recently implicated in diabetes and obesity, prompting attempts to discover new HSL inhibitors. Toward this end, we explored the pharmacophoric space of HSL inhibitors using four ...
- a,b-Methylene-2'-deoxynucleoside 5'-Triphosphates as Noncleavable Substrates for DNA Polymerases: Isolation, Characterization, and Stability Studies of Novel 2'-Deoxycyclonucleosides, 3,5'-Cyclo-dG, and 2,5'-Cyclo-dT.
[作者:Liang, Fengting;Jain, Nidhi;Hutchens, Troy;Shock, David D.;Beard, William A.;Wilson, Samuel H.;Chiarelli, M. Paul;Cho, Bongsup P.;,期刊:Journal of Medicinal Chemistry, 页码:6460-6470 , 文章类型: 研究论文,,卷期:2008年51-20]
- We report synthesis and characterization of a complete set of a,b-methylene-2'-dNTPs (a,b-m-dNTP; N = A, C, T, G, 12-15) in which the a,b-oxygen linkage of natural dNTP was replaced by a methylene group. These nucleotid...
- Structure-Activity Relationships of Truncated D- and L-4'-Thioadenosine Derivatives as Species-Independent A3 Adenosine Receptor Antagonists.
[作者:Jeong, Lak Shin;Pal, Shantanu;Choe, Seung Ah;Choi, Won Jun;Jacobson, Kenneth A.;Gao, Zhan-Guo;Klutz, Athena M.;Hou, Xiyan;Kim, Hea Ok;Lee, Hyuk Woo;Lee, Sang Kook;Tosh, Dilip K.;Moon, Hyung Ryong;,期刊:Journal of Medicinal Chemistry, 页码:6609-6613 , 文章类型: 研究论文,,卷期:2008年51-20]
- Novel D- and L-4'-thioadenosine derivs. lacking the 4'-hydroxymethyl moiety were synthesized, starting from D-mannose and D-gulonic g-lactone, resp., as potent and selective species-independent A3 adenosine receptor (AR)...
- Structure-Activity Studies on a Series of a 2-Aminopyrimidine-Containing Histamine H4 Receptor Ligands.
[作者:Altenbach, Robert J.;Adair, Ronald M.;Bettencourt, Brian M.;Black, Lawrence A.;Fix-Stenzel, Shannon R.;Gopalakrishnan, Sujatha M.;Hsieh, Gin C.;Liu, Huaqing;Marsh, Kennan C.;McPherson, Michael J.;Milicic, Ivan;Miller, Thomas R.;Vortherms, Timothy A.;Warri,期刊:Journal of Medicinal Chemistry, 页码:6571-6580 , 文章类型: 研究论文,,卷期:2008年51-20]
- Compounds (More Than One Hetero Atom)) Section A series of 2-aminopyrimidines, e.g. I (R1 = H, Me, OMe, NH2, Ph; R2 = H, Cl, I, NHMe, NMe2, Ph, 2-MeOC6H4, 1-naphthyl, 4-pyridyl, etc.), was synthesized as ligands of the h...
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