4281-78-1

Upstream product

• 59-88-1 phenylhydrazine hydrochloride 
• 25109-08-4 toluene-4-sulfonic acid 3-(1H-indol-3-yl)propyl ester 
• 35386-24-4 1-(2-Methoxyphenyl)piperazine 
• 3569-21-9 1H-indole-3-propanol 

Relevant academic research and scientific papers

Synthesis, 5-hydroxytryptamine1A receptor affinity and docking studies of 3-[3-(4-aryl-1-piperazinyl)-propyl]-1H-indole derivatives

A series of 3-[3-(4-aryl-1-piperazinyl)-propyl]-1H-indole derivatives (12a-h) was synthesized and evaluated for binding affinity at the human 5-hydroxytryptamine1A receptor (5-HT1AR) compounds (12b) and (12h) showed the highest 5-HT1A receptor affinity (IC 50-=15 nM). Molecular docking studies with all the compounds in a homology model of 5-HT1A showed that the main interaction anchoring the ligand in the receptor was a charge-reinforced bond between the protonated nitrogen atom (N-4) of the piperazine ring and Aspartate3.32.

Piperazinobutyrophenone derivatives

Central nervous system active butyrophenone derivatives in which γ -piperazinobutyrophenone derivatives of the formula, SPC1 Wherein R1 is hydrogen, amino, C1 -C5 alkanoylamino, C1 -C4 alkylamino or N-(C1 -C4 alkyl)(C1 -C5 alkanoyl) amino; R2 is hydrogen or halogen; R3 is hydrogen, halogen, C1 -C4 alkyl, C1 -C4 alkoxy or trifluoromethyl; and m is 0, 1 or 2, and acid addition salts thereof, can be prepared by reacting an indole derivative of the formula, SPC2 Wherein R2, R3 and m are the same as defined above, and R4 and R5 are hydrogen or C1 -C4 alkyl respectively, with an oxidizing agent to yield an o-alkanoylamino-γ-piperazinobutyrophenone derivative of the formula, SPC3 Wherein R2, R3, R4, R5 and m are the same as defined above, and further, if necessary, hydrolyzing the product to yield an o-amino-γ-piperazinobutyrophenone derivative of the formula, SPC4 Wherein R2, R3, R5 and m are the same as defined above, and further diazotizing, if desired, in case R5 is hydrogen, the obtained o-amino-γ-piperazinobutyrophenone derivative and subsequently decomposing the resultant diazonium compound to replace the diazonium group by hydrogen. Among the butyrophenone derivatives thus obtained, those in which R1 is amino, alkanoylamino, alkylamino or N-alkylalkanoylamino and those in which R1 is hydrogen and R2 is halogen substituted at meta-position to carbonyl group are novel compounds.