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, 69451 Weinheim, Germany, 2008)

No abstract

No abstract

String synthesis [1-3] is an efficient and cheap manual method for preparation of combinatorial libraries by using macroscopic solid support units. Sorting the units between two synthetic steps is an important operation of the procedure. The software developed to guide sorting can be used only when complete combinatorial libraries are prepared. Since very often only selected components of the full libraries are needed, new software was constructed that guides sorting in preparation of non-complete combinatorial libraries. Application of the software is described in details.

Pyrazine derivatives R 0550Facile Synthesis of Pyridazine-Based α-Helix Mimetics. -A versatile synthesis of an amphiphilic, nonpeptidic urea-pyridazine-piperazine scaffold [cf. (VII), (VIII)] is presented. The method uses a pyridazine core, and minimizes the number of C-C bond forming reactions. -(MOISAN, L.; DALE, T. J.; GOMBOSUREN, N.; BIROS, S. M.; MANN, E.; HOU, J.-L.; CRISOSTOMO, F. P.; REBEK*, J. J.; Heterocycles 73 (2007) 1, 661-671; Skaggs Inst. Chem. Biol., Scripps Res. Inst.,