- In Vivo Active Aldosterone Synthase Inhibitors with Improved Selectivity: Lead Optimization Providing a Series of Pyridine Substituted 3,4-Dihydro-1H-quinolin-2-one Derivatives.
[作者:Lucas, Simon;Heim, Ralf;Ries, Christina;Schewe, Katarzyna E.;Birk, Barbara;Hartmann, Rolf W.;,期刊:Journal of Medicinal Chemistry, 页码:8077-8087 , 文章类型: 研究论文,,卷期:2008年51-24]
- Pyridine substituted naphthalenes (e.g., I-III) constitute a class of potent inhibitors of aldosterone synthase (CYP11B2). To overcome the unwanted inhibition of the hepatic enzyme CYP1A2, we aimed at reducing the no. o...
- Crystal Structure of the Peroxisome Proliferator-Activated Receptor g (PPARg) Ligand Binding Domain Complexed with a Novel Partial Agonist: A New Region of the Hydrophobic Pocket Could Be Exploited for Drug Design.
[作者:Montanari, Roberta;Saccoccia, Fulvio;Scotti, Elena;Crestani, Maurizio;Godio, Cristina;Gilardi, Federica;Loiodice, Fulvio;Fracchiolla, Giuseppe;Laghezza, Antonio;Tortorella, Paolo;Lavecchia, Antonio;Novellino, Ettore;Mazza, Fernando;Aschi, Massimiliano;Poc,期刊:Journal of Medicinal Chemistry, 页码:7768-7776 , 文章类型: 研究论文,,卷期:2008年51-24]
- The peroxisome proliferator-activated receptors (PPARs) are ligand-dependent transcription factors regulating glucose and lipid metab. The search for new PPAR ligands with reduced adverse effects with respect to the mar...
- Cytochrome P450 2C9 Type II Binding Studies on Quinoline-4-Carboxamide Analogues.
[作者:Peng, Chi-Chi;Cape, Jonathan L.;Rushmore, Tom;Crouch, Gregory J.;Jones, Jeffrey P.;,期刊:Journal of Medicinal Chemistry, 页码:8000-8011 , 文章类型: 研究论文,,卷期:2008年51-24]
- CYP2C9 is a significant P 450 protein responsible for drug metab. With the increased use of heterocyclic compds. in drug design, a rapid and efficient predrug screening of these potential type II binding compds. is essen...
- Further Studies with the 2-Amino-1,3-thiazol-4(5H)-one Class of 11b-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Reducing Pregnane X Receptor Activity and Exploring Activity in a Monkey Pharmacodynamic Model.
[作者:Fotsch, Christopher;Bartberger, Michael D.;Bercot, Eric A.;Chen, Michelle;Cupples, Rod;Emery, Maury;Fretland, Jenne;Guram, Anil;Hale, Clarence;Han, Nianhe;Hickman, Dean;Hungate, Randall W.;Hayashi, Michael;Komorowski, Renee;Liu, Qingyian;Matsumoto, Guy;St,期刊:Journal of Medicinal Chemistry, 页码:7953-7967 , 文章类型: 研究论文,,卷期:2008年51-24]
- A series of compds. contg. the 2-amino-1,3-thiazol-4(5H)-one core were found to be potent inhibitors of the enzyme 11b-hydroxysteroid dehydrogenase type 1 (11b-HSD1). One of our lead compds. from this series activated t...
- Dual Inhibitors of Matrix Metalloproteinases and Carbonic Anhydrases: Iminodiacetyl-Based Hydroxamate-Benzenesulfonamide Conjugates.
[作者:Marques, Sergio M.;Nuti, Elisa;Rossello, Armando;Supuran, Claudiu T.;Tuccinardi, Tiziano;Martinelli, Adriano;Santos, M. Amelia;,期刊:Journal of Medicinal Chemistry, 页码:7968-7979 , 文章类型: 研究论文,,卷期:2008年51-24]
- Matrix metalloproteinases (MMPs) and carbonic anhydrases (CAs) are two classes of zinc enzymes with different roles and catalytic targets, such as the degrdn. of most of the extracellular matrix (ECM) proteins and the re...
- Discovery of Quinazolines as Histamine H4 Receptor Inverse Agonists Using a Scaffold Hopping Approach.
[作者:Smits, Rogier A.;de Esch, Iwan J. P.;Zuiderveld, Obbe P.;Broeker, Joachim;Sansuk, Kamonchanok;Guaita, Elena;Coruzzi, Gabriella;Adami, Maristella;Haaksma, Eric;Leurs, Rob;,期刊:Journal of Medicinal Chemistry, 页码:7855-7865 , 文章类型: 研究论文,,卷期:2008年51-24]
- From a series of small fragments that was designed to probe the histamine H4 receptor (H4R), we previously described quinoxaline-contg. fragments that were grown into high affinity H4R ligands in a process that was guide...
- Pirinixic Acid Derivatives as Novel Dual Inhibitors of Microsomal Prostaglandin E2 Synthase-1 and 5-Lipoxygenase.
[作者:Koeberle, Andreas;Zettl, Heiko;Greiner, Christine;Wurglics, Mario;Schubert-Zsilavecz, Manfred;Werz, Oliver;,期刊:Journal of Medicinal Chemistry, 页码:8068-8076 , 文章类型: 研究论文,,卷期:2008年51-24]
- Dual inhibition of the prostaglandin (PG) and leukotriene (LT) biosynthetic pathway is supposed to be superior over single interference, both in terms of efficacy and side effects. Here, we present a novel class of dual...
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