552885-53-7

Upstream product

• 686710-22-5 (+/-)-1-[1-(4-fluorophenyl)-2-piperazin-1-ylethyl]-4-isopropylpiperazine 
• 19853-17-9 3-(biphenyl-2-yl)propanoic acid 
• 106000-09-3 1-<2-Chloro-2-(4-fluorophenyl)ethyl>-4-ethoxycarbonylpiperazine 
• 89011-47-2 ethyl 4-[2-(4-fluorophenyl)-2-hydroxyethyl]piperazine-1-carboxylate hydrochloride 
• 552885-52-6 ethyl 4-[2-(4-fluorophenyl)-2-(4-isopropylpiperazin-1-yl)ethyl]piperazine-1-carboxylate 

Downstream Products

• 552885-54-8 1-[2-(4-fluorophenyl)-2-(4-isopropylpiperazino)ethyl]-4-(3-biphenyl-2-ylpropyl)-piperazine 

Relevant academic research and scientific papers

Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor

During the investigation of antagonists for the MC4 receptor, we found that 10ab having a naphthyl group showed almost the same binding affinity for the MC4 receptor as that of the lead compound 1 with a benzoyl group. We also developed a new type of compounds, namely, bis-piperazines, and found that the bis-piperazines 10 exhibited a high affinity for the MC4 receptor. In particular, (-)-10bg exhibited the highest affinity for the MC4 receptor with an IC50 value of 8.13 nM. In this paper, we present the design, synthesis, and structure-activity relationships of the novel bis-piperazines as MC4 receptor antagonists.

PIPERAZINE DERIVATIVE

A piperazine derivative represented by the formula (1): ???wherein n is an integer of 1 to 8; R1 represents hydrogen or C1-10 alkyl; A represents CH or nitrogen; Ar1 represents phenyl or substituted phenyl; and Y represents a group represented by the formula Y1-Y2-Ar2 or Y3-Y4(Ar5)-Ar6 or a pharmaceutically acceptable salt of the derivative. The novel piperazine derivative has MC4 receptor antagonistic activity.