244289-94-9Relevant academic research and scientific papers
Low-Molecular-Weight CXCR4 Ligands with Variable Spacers
Narumi, Tetsuo,Aikawa, Haruo,Tanaka, Tomohiro,Hashimoto, Chie,Ohashi, Nami,Nomura, Wataru,Kobayakawa, Takuya,Takano, Hikaru,Hirota, Yuki,Murakami, Tsutomu,Yamamoto, Naoki,Tamamura, Hirokazu
supporting information, p. 118 - 124 (2013/02/26)
Low-molecular-weight CXCR4 ligands based on known lead compounds including the 14-mer peptide T140, the cyclic pentapeptide FC131, peptide mimetics, and dipicolylamine-containing compounds were designed and synthesized. Three types of aromatic spacers, 1,4-phenylenedimethanamine, naphthalene-2,6-diyldimethanamine, and [1,1′-biphenyl]-4,4′-diyldimethanamine, were used to build four pharmacophore groups. As pharmacophore groups, 2-pyridylmethyl and 1-naphthylmethyl are present in all of the compounds, and several aromatic groups and a cationic group from 1-propylguanidine and 1,1,3,3-tetramethyl-2-propylguanidine were also used. Several compounds showed significant CXCR4 binding affinity, and zinc(II) complexation of bis(pyridin-2-ylmethyl)amine moieties resulted in a remarkable increase in CXCR4 binding affinity.
Pharmacophore-based small molecule CXCR4 ligands
Narumi, Tetsuo,Tanaka, Tomohiro,Hashimoto, Chie,Nomura, Wataru,Aikawa, Haruo,Sohma, Akira,Itotani, Kyoko,Kawamata, Miyako,Murakami, Tsutomu,Yamamoto, Naoki,Tamamura, Hirokazu
scheme or table, p. 4169 - 4172 (2012/07/03)
Low molecular weight CXCR4 ligands were developed based on the peptide T140, which has previously been identified as a potent CXCR4 antagonist. Some compounds with naphthyl, fluorobenzyl and pyridyl moieties as pharmacophore groups in the molecule showed significant CXCR4-binding activity and anti-HIV activity. Structure-activity relationships were studied and characteristics of each of these three moieties necessary for CXCR4 binding were defined. In this way, CXCR4 ligands with two types of recognition modes for CXCR4 have been found.
New amide derivatives as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity
Cirauqui, Nuria,Ceras, Javier,Galiano, Silvia,Perez-Silanes, Silvia,Juanenea, Laura,Rivera, Gildardo,Aldana, Ignacio,Monge, Antonio
experimental part, p. 585 - 591 (2009/04/06)
Melanin-concentrating hormone (MCH) is a recently discovered central nervous system (CNS) target for treating obesity. Two novel series of amide derivatives were synthesized and evaluated biologically as MCH-R1 (melanin-concentrating hormone receptor 1) antagonists. The results showed that diphenyl substituents on the amide lead to better activity than biphenyl substituents. ECV Editio Cantor Verlag.
