521917-66-8Relevant articles and documents
Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: Potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis
Voets, Marieke,Antes, Iris,Scherer, Christiane,Müller-Vieira, Ursula,Biemel, Klaus,Marchais-Oberwinkler, Sandrine,Hartmann, Rolf W.
, p. 2222 - 2231 (2007/10/03)
In this study, the synthesis and biological evaluation of heteroaryl-substituted dihydronaphthalenes and indenes (1-16) is described. The compounds were tested for activity by use of human CYP11B2 expressed in fission yeast and V79 MZh cells and for selectivity by use of human CYP11B1, CYP17, and CYP19. The most active inhibitor was the 6-methoxydihydronaphthalene 4 (IC 50 = 2 nM), showing a Ki value of 1.3 nM and a competitive type of inhibition. The 5-methoxyindene 3 was found to be the most selective CYP11B2 inhibitor (IC50 = 4 nM; CYP11B1 IC50 = 5684 nM), which also showed only marginal inhibition of human CYP3A4 and CYP2D6. Docking and molecular dynamics studies using our homology-modeled CYP11B2 structure were performed to understand some structure-activity relationships. Caco-2 cell experiments revealed highly cell-permeable compounds, and metabolic studies with 4 using rat liver microsomes showed sufficient stability.
2-Styryl-pyridines and 2-(3,4-Dihydro-naphthalen-2-yl)-pyridines as potent NR1/2B subtype selective NMDA receptor antagonists
Buettelmann, Bernd,Alanine, Alexander,Bourson, Anne,Gill, Ramanjit,Heitz, Marie-Paule,Mutel, Vincent,Pinard, Emmanuel,Trube, Gerhard,Wyler, Rene
, p. 630 - 633 (2007/10/03)
A series of 2-styryl-pyridines and 2-(3,4-dihydro-naphthalen-2-yl)- pyridines was prepared and evaluated as NR1/2B subtype selective NMDA receptor antagonists. The SAR developed in this series resulted in the discovery of high affinity antagonists that are selective (vs. α1 and M 1 receptors) and are active in vivo.
Substituted imidazol-pyridazine derivatives
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Page 23, (2010/02/05)
The present invention relates to compounds of formula wherein A is an unsubstituted or substituted cyclic group; and R is hydrogen or lower alkyl; or a pharmaceutically acceptable acid addition salt thereof. These compounds are NMDA NR-2B receptor subtype specific blockers and are useful in the treatment of neurodegeneration, depression and pain.
Conjugated aromatic compounds with a pyridine substituent
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, (2008/06/13)
The present invention relates to compounds of formulae The compounds of the present invention are NMDA (N-methyl-D-aspartate)-receptor subtype blockers and are used in the treatment of diseases related to this receptor.