247206-81-1Relevant articles and documents
Design and synthesis of Rho kinase inhibitors (II)
Iwakubo, Masayuki,Takami, Atsuya,Okada, Yuji,Kawata, Takehisa,Tagami, Yoshimichi,Ohashi, Hiroshi,Sato, Motoko,Sugiyama, Terumi,Fukushima, Kayoko,Iijima, Hiroshi
, p. 350 - 364 (2008/02/04)
In a previous study, we identified several structurally unrelated scaffolds of the Rho kinase inhibitor using pharmacophore information obtained from the results of a high-throughput screening and structural information from a homology model of Rho kinase. 1H-Indazole is one of the candidate scaffolds on which a new series of potent Rho kinase inhibitors could be developed. In this study, the detailed structure-activity relationship of 1H-indazole analogues was studied. During this study, we found that the cell-free enzyme inhibitory potential of Rho kinase inhibitors having the 1H-indazole scaffold did not necessarily correlate with their inhibitory potential toward the chemotaxis of cultured cells. The choice of the linker substructure was shown to be an important factor for the 1H-indazole analogues to inhibit the chemotaxis of cells. Optimization of the 1H-indazole inhibitors with respect to the in vitro inhibition of monocyte chemotaxis induced by MCP-1 was carried out. The inhibitory potential was improved both in the cell-free enzyme assay and in the chemotaxis assay.
PESTICIDAL SUBSTITUTED PIPERIDINES
-
Page/Page column 51, (2008/06/13)
The invention relates to the use of piperidine derivatives encompassed from the general formula (I) for the control of pests, including arthropods and helminths, and a method for the control of pests.
Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1, adenosine receptor
Baraldi, Pier Giovanni,Romagnoli, Romeo,Pavani, Maria Giovanna,Del Carmen Nu?ez, Maria,Tabrizi, Mojgan Aghazadeh,Shryock, John C.,Leung, Edward,Moorman, Allan R.,Uluoglu, Canan,Iannotta, Valeria,Merighi, Stefania,Borea, Pier Andrea
, p. 794 - 809 (2007/10/03)
The current study describes the synthesis and biological evaluation of a novel series of 2-amino-3-naphthoylthiophenes, with variable modifications at the 4- and 5-position of the thiophene as well as the naphthoyl ring. Allosteric enhancer activity was m
Allosteric modulation of the adenosine A1 receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding
Van Der Klein, Pieter A. M.,Kourounakis, Angeliki P.,IJzerman, Ad P.
, p. 3629 - 3635 (2007/10/03)
Novel allosteric enhancers of agonist binding to the rat adenosine A1 receptor are described. The lead compound for the new series was PD 81,723 ((2-amino-4,5-dimethyl-3-thienyl)[3-(trifluoromethyl)phenyl]methanone), a compound previously reported by Bruns and co-workers (Mol. Pharmacol. 1990, 38, 950-958). The 4,5-dimethyl group and the benzoyl moiety were targets for further modifications, leading to series of 4,5-dialkyl (12a-g), of tetrahydrobenzo (12h-u), and of tetrahydropyridine (13a-g) derivatives. A number of compounds, in particular 12b, 12e, 12j, 12n, and 12u, proved superior to PD 81,723. Their EC50 values for enhancing the binding of the adenosine A1 receptor agonist N6-cyclopentyladenosine to the receptor were lower, and/or their antagonistic activity on the adenosine A1 receptor was shown to be diminished.