835595-64-7Relevant academic research and scientific papers
CCR5 antagonists as anti-HIV-1 agents. Part 3: Synthesis and biological evaluation of piperidine-4-carboxamide derivatives
Imamura, Shinichi,Nishikawa, Youichi,Ichikawa, Takashi,Hattori, Taeko,Matsushita, Yoshihiro,Hashiguchi, Shohei,Kanzaki, Naoyuki,Iizawa, Yuji,Baba, Masanori,Sugihara, Yoshihiro
, p. 397 - 416 (2007/10/03)
Replacement of the 5-oxopyrrolidin-3-yl fragment in the previously reported lead structure with a 1-acetylpiperidin-4-yl group led to the discovery of a novel series of potent CCR5 antagonists. Introduction of small hydrophobic substituents on the central phenyl ring increased the binding affinity, providing low to sub-nanomolar CCR5 antagonists. The selected compound 11f showed excellent antiviral activity against CCR5-using HIV-1 replication in human peripheral blood mononuclear cells (EC50 = 0.59 nM) and an acceptable pharmacokinetic profile in dogs.
The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists
Ting, Pauline C.,Lee, Joe F.,Wu, Jie,Umland, Shelby P.,Aslanian, Robert,Cao, Jianhua,Dong, Youhao,Garlisi, Charles G.,Gilbert, Eric J.,Huang, Ying,Jakway, James,Kelly, Joseph,Liu, Zhidan,McCombie, Stuart,Shah, Himanshu,Tian, Fang,Wan, Yuntao,Shih, Neng-Yang
, p. 1375 - 1378 (2007/10/03)
Bipiperidine amide 1 has been identified as a CC chemokine receptor 3 (CCR3) antagonist. Optimization of its structure-activity relationship has resulted in the identification of cis (R,R)-4-[(3,4-dichlorophenyl)methyl]-3- hydroxymethyl-1′(6-quinolinylcar
