859832-27-2

Upstream product

• 174574-69-7 4-chloro-3-(1H-indol-3-yl)-1-methyl-1H-pyrrole-2,5-dione 
• 859832-21-6 3-(4-chloro-1-methyl-2,5-dihydro-1H-pyrrol-3-yl)-1H-indole 
• 98-58-8 4-bromobenzenesulfonyl chloride 
• 1123-61-1 3,4-dichloro-1-methyl-pyrrole-2,5-dione 

Relevant academic research and scientific papers

Rigidized 1-aryl sulfonyl tryptamines: Synthesis and pharmacological evaluation as 5-HT6 receptor ligands

A series of N1-arylsulfonyl-3-(pyrrolidin-3-yl)-1H-indole and N1-arylsulfonyl-3-(4-chloro-2,5-dihydro-1H-pyrrol-3-yl)-1H-indole derivatives (tryptamine derivatives with rigidized side chain) have been prepared and tested for their binding affinity to 5-HT6 receptor. Several compounds displayed potent binding affinity for the 5-HT6 receptor when tested in in vitro binding assay. The primary SAR indicates that rigidification of dimethylamino alkyl chain at C3 of indole carbon maintains the binding affinity to 5-HT6R. The lead compound N 1-benzenesulfonyl-3-(4-chloro-1-methyl-2,5-dihydro-1H-pyrrol-3-yl) -1H-indole, 10a (Kb = 0.1 nM) has shown excellent in vitro affinity and was active in animal models of cognition like NORT and water maze.

3-(PYROLIDIN-3-L) INDOLES AS 5-HT6 RECEPTOR MODULATORS

The present invention describes 3-(Heterocyclic)indoles with the Formula (I), its stereoisomers and salts, wherein the substituents such as R, R1, R2, R3, R4, R10, R11, R12, R13, and R14 are described in the specification. The invention also provides a method to prepare compound with formula (I), pharmaceutical composition containing such compounds and method to manufacture a medicament. These compounds are useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory disease, genito-urological disorders, cardio vascular diseases and cancer.