932028-02-9Relevant articles and documents
Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor
Nozawa, Dai,Okubo, Taketoshi,Ishii, Takaaki,Kakinuma, Hiroyuki,Chaki, Shigeyuki,Okuyama, Shigeru,Nakazato, Atsuro
, p. 1989 - 2005 (2007/10/03)
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.