1007396-24-8Relevant academic research and scientific papers
Synthesis of an oxazole-pyrrole-piperazine scaffold as an α-helix mimetic
Moisan, Lionel,Odermatt, Severin,Gombosuren, Naran,Carella, Alexandre,Rebek Jr., Julius
, p. 1673 - 1676 (2008)
The synthesis of nonpeptidic α-helix mimetics based on a tricyclic oxazole-pyrrole-piperazine scaffold is described. The scaffold presents both a hydrophobic surface for recognition and a hydrophilic edge that enhances solubility. The synthesis is highly modular and allows the targeting of a range of protein-protein interactions involving α-helices. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
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
, p. 661 - 671 (2007)
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.
UPP AMPHIPHILIC ALPHA-HELIX MIMETICS
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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.
