Synthesis and structure–activity relationship of RXR antagonists based on the diazepinylbenzoic acid structure

Synthesis and structure–activity relationship of RXR antagonists based on the diazepinylbenzoic acid structure

Synthesis and structure–activity relationship of RXR antagonists employing a diazepinylbenzoic acid scaffold are described. The sulfonamide derivatives were found to reveal a high antagonistic activity and good pharmacokinetic properties. Synthesis and structure–activity relationship of RXR antagoni...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2007-09, Vol.17 (17), p.4808-4811
Hauptverfasser: Sakaki, Junichi, Konishi, Kazuhide, Kishida, Masashi, Gunji, Hiroki, Kanazawa, Takanori, Uchiyama, Hidefumi, Fukaya, Hiroaki, Mitani, Hironobu, Kimura, Masaaki
Format: Artikel
Sprache:eng
Schlagworte:
Administration, Oral
Antagonist
Benzoates - chemical synthesis
Benzoates - chemistry
Biological and medical sciences
Biphenyl Compounds - chemical synthesis
Biphenyl Compounds - chemistry
Chemistry, Pharmaceutical - methods
Diazepinylbenzoic acid
Drug Design
Humans
Inhibitory Concentration 50
Medical sciences
Miscellaneous
Models, Chemical
Molecular Structure
Pharmacology. Drug treatments
Receptors, Retinoic Acid - antagonists & inhibitors
Receptors, Retinoic Acid - chemistry
Retinoic Acid Receptor alpha
RXR
Structure-Activity Relationship
Time Factors
Trans-Activators
Transcription Factors - chemistry
Transcriptional Activation
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Zusammenfassung:Synthesis and structure–activity relationship of RXR antagonists employing a diazepinylbenzoic acid scaffold are described. The sulfonamide derivatives were found to reveal a high antagonistic activity and good pharmacokinetic properties. Synthesis and structure–activity relationship of RXR antagonists employing a diazepinylbenzoic acid scaffold are described. Of those antagonists, sulfonamide derivatives ( 6v and 6w) reveal a high antagonistic activity and good pharmacokinetic properties.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.06.079