1001289-56-0

Upstream product

• 10297-06-0 1-chloro-5-hexyne 
• 121-33-5 vanillin 
• 76911-01-8 5-hexynyl p-toluenesulfonate 

Downstream Products

• 1311157-65-9 1-({4-[4-(1-butyl-1H-1,2,3-triazole-4-yl)butoxy]-3-methoxyphenyl}methyl)-4-(2-methoxyphenyl)piperazine 
• 1311157-62-6 4-[4-(1-butyl-1H-1,2,3-triazole-4-yl)butoxy]-3-methoxybenzaldehyde 
• 1311157-54-6 4,4'-[decane-1,10-diylbis(1H-1,2,3-triazole-1,4-diylbutane-4,1-diyloxy)]bis(3-methoxybenzaldehyde) 
• 1311157-47-7 1,1'-{decane-1,10-diylbis[1H-1,2,3-triazole-1,4-diylbutane-4,1-diyloxy(3-methoxy-4,1-phenylene)methylene]}bis[4-(2-methoxyphenyl)piperazine] 

Relevant academic research and scientific papers

Bivalent dopamine D2 receptor ligands: Synthesis and binding properties

Dopamine D2 receptor homodimers might be of particular importance in the pathophysiology of schizophrenia and, thus, serve as promising target proteins for the discovery of atypical antipsychotics. A highly attractive approach to investigate and control GPCR dimerization may be provided by the exploration and characterization of bivalent ligands, which can act as molecular probes simultaneously binding two adjacent binding sites of a dimer. The synthesis of bivalent dopamine D2 receptor ligands of type 1 is presented, incorporating the privileged structure of 1,4-disubstituted aromatic piperidines/piperazines (1,4-DAPs) and triazolyl-linked spacer elements. Radioligand binding studies provided diagnostic insights when Hill slopes close to two for bivalent ligands with particular spacer lengths and a comparative analysis with respective monovalent control ligands and unsymmetrically substituted analogues indicated a bivalent binding mode with a simultaneous occupancy of two neighboring binding sites.

Evaluation and optimization of antifibrotic activity of cinnamoyl anthranilates

Tranilast is an anti-inflammatory drug in use for asthma and atopic dermatitis. In studies over the last decade it has been revealed that tranilast can reduce fibrosis occurring in the kidney during diabetes, thereby delaying and/or preventing kidney dysfunction. We report a structure-activity study aimed at optimizing the antifibrotic activity of tranilast. A series of cinnamoyl anthranilates were prepared and assessed for their ability to prevent TGF-β-stimulated production of collagen in cultured renal mesangial cells. We reveal derivatives with improved potency and reduced cellular toxicity relative to tranilast. 3-Methoxy-4-propargyloxycinnamoyl anthranilate reduces albuminuria in a rat model of progressive diabetes, and thus has potential as an innovative treatment for diabetic nephropathy.

THERAPEUTIC COMPOUNDS

Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof; with the proviso that the compound is not Tranilast.