1007396-25-9Relevant academic research and scientific papers
UPP AMPHIPHILIC ALPHA-HELIX MIMETICS
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Page/Page column 12-13; Sheet 2/4, (2009/04/25)
Functionalized pyridazine derivatives having a low molecular weight and pharmaceutical compositions thereof are useful as alpha-helical mimetics for efficiently disrupting protein-protein interactions such as Bak/Bcl-XL, p53/HDM2, calmodulin/smooth muscle myosin light-chain kinase, and gp41 assembly and for treating conditions and/or disorders mediated by disruption of alpha-helix-binding receptors and proteins.
Synthesis of pyridazines functionalized with amino acid side chains
Mann, Enrique,Moisan, Lionel,Hou, Jun-Li,Rebek Jr., Julius
, p. 903 - 905 (2008/09/17)
A simple route for the preparation of 3,4,6-substituted pyridazines is described by using Tebbe olefination of esters then Diels-Alder reaction of the resulting enol ethers with tetrazine.
Facile Synthesis of Pyridazine-based α-Helix Mimetrics
Moisan, Lionel,Dale, Trevor J.,Gombosuren, Naran,Biros, Shannon M.,Mann, Enrique,Hou, Jun-Li,Crisostomo, Fernando P.,Jr., Julius Rebek
experimental part, p. 661 - 671 (2009/09/28)
The synthesis of an amphiphilic, nonpeptidic scaffold that mimics the presentation of i, i+4, and i+7 residues of an α-helix is presented. The approach uses a pyridazine core, and minimizes the number of C-C bond forming reactions. The synthesis of this Urea-Pyridazine-Piperazine (UPP) scaffold is versatile and its synthesis makes it suitable for the preparationof small libraries of low-molecular-weight α-helix mimetics that can be targeted to specific protein/protein interactions.
