412049-71-9

Usage

Chemical compound

1H-Indole, 1-(phenylsulfonyl)-4-(1-piperazinyl)-

Indole ring

A five-membered aromatic ring system with a nitrogen atom at position 1

Substitution

The indole ring is substituted with a sulfonylphenyl group at position 1 and a piperazinyl group at position 4

Sulfonylphenyl group

A phenyl ring connected to a sulfonyl group (-SO2-) which is a common pharmacophore in drug design

Piperazinyl group

A five-membered heterocyclic ring with two nitrogen atoms, often used as a bioisostere for other functional groups in medicinal chemistry

Potential biological activities

The compound has been studied for its potential as an antipsychotic agent and its activity on various neurotransmitter receptors

Molecular structure

The compound's molecular structure and potential interactions with biological targets make it an interesting candidate for further research and development in the field of medicinal chemistry.

Upstream product

• 98-09-9 benzenesulfonyl chloride 
• 676448-17-2 4-bromoindole-1-carboxylic acid tert-butyl ester 
• 252978-89-5 4-(1H-indol-4-yl)-piperazine-1-carboxylic acid tert-butyl ester 
• 393508-48-0 4-(1-benzenesulfonyl-1H-indol-4-yl)-piperazine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties

The complex etiology of Alzheimer's disease has initiated a quest for multi-target ligands to address the multifactorial causes of this neurodegenerative disorder. In this context, we designed dual-acting 5-HT6 receptor (5-HT6R) anta

Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT 6 receptor antagonists

Starting from the potent and selective but poorly brain penetrant 5-HT 6 receptor antagonist SB-271046, a successful strategy for improving brain penetration was adopted involving conformational constraint with concomitant reduction in hydrogen bond count. This provided a series of bicyclic heteroarylpiperazines with high 5-HT6 receptor affinity. 5-Chloroindole 699929 combined high 5-HT6 receptor affinity with excellent brain penetration and also had good oral bioavailability in both rat and dog.

4-piperazinylindole derivatives with 5-HT6 receptor affinity

This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein R3 is SO2—Ar, Ar is aryl or heteroaryl; and R1, R2, R4 and R5 /su

Novel compounds, their use and preparation

The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.

1-Aryl- or 1-alkylsulfonyl-heterocyclylbenzazoles as 5-hydroxytryptamine-6 ligands

The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.