- Discovery of (R)-4-(8-Fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1 H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)pipe ridine-1-carboxamide (BMS-694153): A Potent Antagonist of the Human Calcitonin Gene-Related Pept
[作者：Degnan, Andrew P.;Chaturvedula, Prasad V.;Conway, Charles M.;Cook, Deborah A.;Davis, Carl D.;Denton, Rex;Han, Xiaojun;Macci, Robert;Mathias, Neil R.;Moench, Paul;Pin, Sokhom S.;Ren, Shelly X.;Schartman, Richard;Signor, Laura J.;Thalody, George;Widmann, Ki,期刊：Journal of Medicinal Chemistry, 页码：4858-4861 , 文章类型： 研究论文，,卷期：2008年51-16]
- Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Early chem. leads suffered from modest potency, significant CYP3A4 inhibition, and poor aq. soly. Herein, we describe the opti...
- 3-(1H-Tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): A Partial Agonist of the Nicotinic Acid Receptor, G-Protein Coupled Receptor 109a, with Antilipolytic but No Vasodilatory Activity in Mice.
[作者：Semple, Graeme;Skinner, Philip J.;Gharbaoui, Tawfik;Shin, Young-Jun;Jung, Jae-Kyu;Cherrier, Martin C.;Webb, Peter J.;Tamura, Susan Y.;Boatman, P. Douglas;Sage, Carleton R.;Schrader, Thomas O.;Chen, Ruoping;Colletti, Steven L.;Tata, James R.;Waters, M. Ger,期刊：Journal of Medicinal Chemistry, 页码：5101-5108 , 文章类型： 研究论文，,卷期：2008年51-16]
- The discovery and profiling of 3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (5a, MK-0354), a partial agonist of GPR109a, is described. Compd. 5a retained the plasma free fatty acid lowering effects in mice...
- A Click Chemistry Approach to Pleuromutilin Conjugates with Nucleosides or Acyclic Nucleoside Derivatives and Their Binding to the Bacterial Ribosome.
[作者：Lolk, Line;Pohlsgaard, Jacob;Jepsen, Anne Sofie;Hansen, Lykke H.;Nielsen, Henrik;Steffansen, Signe I.;Sparving, Laura;Nielsen, Annette B.;Vester, Birte;Nielsen, Poul;,期刊：Journal of Medicinal Chemistry, 页码：4957-4967 , 文章类型： 研究论文，,卷期：2008年51-16]
- Pleuromutilin and its derivs. are antibacterial drugs that inhibit protein synthesis in bacteria by binding to ribosomes. To promote rational design of pleuromutilin based drugs, 19 pleuromutilin conjugates with differe...
- Overcoming Undesirable CYP1A2 Inhibition of Pyridylnaphthalene-Type Aldosterone Synthase Inhibitors: Influence of Heteroaryl Derivatization on Potency and Selectivity.
[作者：Heim, Ralf;Lucas, Simon;Grombein, Cornelia M.;Ries, Christina;Schewe, Katarzyna E.;Negri, Matthias;Muller-Vieira, Ursula;Birk, Barbara;Hartmann, Rolf W.;,期刊：Journal of Medicinal Chemistry, 页码：5064-5074 , 文章类型： 研究论文，,卷期：2008年51-16]
- Recently, the authors reported on the development of potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis. A major drawback of these non...
- Structural Basis for the Improved Drug Resistance Profile of New Generation Benzophenone Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors.
[作者：Ren, Jingshan;Chamberlain, Philip P.;Stamp, Anna;Short, Steven A.;Weaver, Kurt L.;Romines, Karen R.;Hazen, Richard;Freeman, Andrew;Ferris, Robert G.;Andrews, C. Webster;Boone, Lawrence;Chan, Joseph H.;Stammers, David K.;,期刊：Journal of Medicinal Chemistry, 页码：5000-5008 , 文章类型： 研究论文，,卷期：2008年51-16]
- Owing to the emergence of resistant virus, next generation non-nucleoside HIV reverse transcriptase inhibitors (NNRTIs) with improved drug resistance profiles have been developed to treat HIV infection. Crystal structur...
- Novel Ligands Rationally Designed for Characterizing I2-Imidazoline Binding Sites Nature and Functions.
[作者：Gentili, Francesco;Cardinaletti, Claudia;Vesprini, Cristian;Ghelfi, Francesca;Farande, Aniket;Giannella, Mario;Piergentili, Alessandro;Quaglia, Wilma;Mattioli, Laura;Perfumi, Marina;Hudson, Alan;Pigini, Maria;,期刊：Journal of Medicinal Chemistry, 页码：5130-5134 , 文章类型： 研究论文，,卷期：2008年51-16]
- The study of two series of 2-aryl-ethylen-imidazolines 3-7 and 8-12 inspired by I2-IBS ligands phenyzoline (1) and diphenyzoline (2), resp., confirmed the interesting "pos." or "neg." morphine analgesia modulation displa...
- Determination of log D via automated microfluidic liquid-liquid extraction.
[作者：Alimuddin, Muhammad;Grant, Daniel;Bulloch, Daryl;Lee, Noelle;Peacock, Martin;Dahl, Russell;,期刊：Journal of Medicinal Chemistry, 页码：5140-5142 , 文章类型： 研究论文，,卷期：2008年51-16]
- A method for log D (pH 7.4) measurement was developed using microfluidic liq.-liq. extn. Values were detd. for 26 compds. and compared to results obtained via shake-flask methods. Excellent correlation between the valu...
- Structure Based Development of Phenylimidazole-Derived Inhibitors of Indoleamine 2,3-Dioxygenase.
[作者：Kumar, Sanjeev;Jaller, Daniel;Patel, Bhumika;LaLonde, Judith M.;DuHadaway, James B.;Malachowski, William P.;Prendergast, George C.;Muller, Alexander J.;,期刊：Journal of Medicinal Chemistry, 页码：4968-4977 , 文章类型： 研究论文，,卷期：2008年51-16]
- Indoleamine 2,3-dioxygenase (IDO) is emerging as an important new therapeutic target for the treatment of cancer, chronic viral infections, and other diseases characterized by pathol. immune suppression. With the goal of...
- Synthesis, Stereochemical Identification, and Selective Inhibitory Activity against Human Monoamine Oxidase-B of 2-Methylcyclohexylidene-(4-arylthiazol-2-yl)hydrazones.
[作者：Chimenti, Franco;Maccioni, Elias;Secci, Daniela;Bolasco, Adriana;Chimenti, Paola;Granese, Arianna;Carradori, Simone;Alcaro, Stefano;Ortuso, Francesco;Yanez, Matilde;Orallo, Francisco;Cirilli, Roberto;Ferretti, Rosella;La Torre, Francesco;,期刊：Journal of Medicinal Chemistry, 页码：4874-4880 , 文章类型： 研究论文，,卷期：2008年51-16]
- A series of 2-methylcyclohexylidene-(4-arylthiazol-2-yl)hydrazones I (R = H, 4-Cl, 4-OMe, etc.) have been investigated for their ability to inhibit selectively the activity of the human A and B isoforms of monoamine oxid...
- Synthesis and Biological Properties of Benzothiazole, Benzoxazole, and Chromen-4-one Analogues of the Potent Antitumor Agent 2-(3,4-Dimethoxyphenyl)-5-fluorobenzothiazole (PMX 610, NSC 721648).
[作者：Aiello, Stefania;Wells, Geoffrey;Stone, Erica L.;Kadri, Hachemi;Bazzi, Rana;Bell, David R.;Stevens, Malcolm F. G.;Matthews, Charles S.;Bradshaw, Tracey D.;Westwell, Andrew D.;,期刊：Journal of Medicinal Chemistry, 页码：5135-5139 , 文章类型： 研究论文，,卷期：2008年51-16]
- New fluorinated 2-arylbenzothiazoles, -benzoxazoles, and -chromen-4-ones were synthesized and their activity against MCF-7 and MDA 468 breast cancer cell lines compared with the potent antitumor benzothiazole I. Analogs...
- Investigations on the 4-quinolone-3-carboxylic acid motif. 2. synthesis and structure-activity relationship of potent and selective cannabinoid-2 receptor agonists endowed with analgesic activity in vivo.
[作者：Pasquini, Serena;Botta, Lorenzo;Semeraro, Teresa;Mugnaini, Claudia;Ligresti, Alessia;Palazzo, Enza;Maione, Sabatino;Di Marzo, Vincenzo;Corelli, Federico;,期刊：Journal of Medicinal Chemistry, 页码：5075-5084 , 文章类型： 研究论文，,卷期：2008年51-16]
- Quinolone-3-carboxamides bearing at position 5, 6, 7, or 8 diverse substituents such as halides, alkyl, aryl, alkoxy, and aryloxy groups differing in their steric/electronic properties, were prepd. The new compds. were ...
- Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 1. Synthesis and Structure-Activity Relationship of a Class of Human Immunodeficiency Virus type 1 Integrase Inhibitors.
[作者：Pasquini, Serena;Mugnaini, Claudia;Tintori, Cristina;Botta, Maurizio;Trejos, Alejandro;Arvela, Riina K.;Larhed, Mats;Witvrouw, Myriam;Michiels, Martine;Christ, Frauke;Debyser, Zeger;Corelli, Federico;,期刊：Journal of Medicinal Chemistry, 页码：5125-5129 , 文章类型： 研究论文，,卷期：2008年51-16]
- A set of 4-quinolone-3-carboxylic acids bearing different substituents on the condensed benzene ring, e.g. I [R = MeOCH2CH2, Me2NCH2CH2, HO(CH2)n, n = 2, 3, 4, etc.], was designed and synthesized as potential HIV-1 integ...
- Discovery and Optimization of a Novel Series of N-Arylamide Oxadiazoles as Potent, Highly Selective and Orally Bioavailable Cannabinoid Receptor 2 (CB2) Agonists.
[作者：Cheng, Yuan;Albrecht, Brian K.;Brown, James;Buchanan, John L.;Buckner, William H.;DiMauro, Erin F.;Emkey, Renee;Fremeau, Robert T.;Harmange, Jean-Christophe;Hoffman, Beth J.;Huang, Liyue;Huang, Ming;Lee, Josie Han;Lin, Fen-Fen;Martin, Matthew W.;Nguyen, H,期刊：Journal of Medicinal Chemistry, 页码：5019-5034 , 文章类型： 研究论文，,卷期：2008年51-16]
- The CB2 receptor is an attractive therapeutic target for analgesic and anti-inflammatory agents. Herein we describe the discovery of a novel class of oxadiazole derivs. from which potent and selective CB2 agonist leads ...
- Discovery of Novel and Long Acting Muscarinic Acetylcholine Receptor Antagonists.
[作者：Jin, Jian;Wang, Yonghui;Shi, Dongchuan;Wang, Feng;Davis, Roderick S.;Jin, Qi;Fu, Wei;Foley, James J.;Webb, Edward F.;Dehaas, Chris J.;Berlanga, Manuela;Burman, Miriam;Sarau, Henry M.;Morrow, Dwight M.;Rao, Parvathi;Kallal, Lorena A.;Moore, Michael L.;Rive,期刊：Journal of Medicinal Chemistry, 页码：4866-4869 , 文章类型： 研究论文，,卷期：2008年51-16]
- discovery of novel quaternary ammonium salts as highly potent muscarinic acetylcholine receptor antagonists with excellent selectivity. Compds. (I, II, and III) showed excellent inhibitory activity and long duration of a...
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