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Antibiotics Antibiotics U 1200 Amide Analogues of TSA: Synthesis, Binding Mode Analysis and HDAC Inhibition. -The synthesis of new amide analogues (VII) and (VIII) of the natural product trichostatin A (TSA) and their evaluation as histone deacetylase (HDAC) inhibitors is described. -(VAN OMMESLAEGHE, K.; ELAUT, G.; BRECX, V.; PAPELEU, P.; ITERBEKE, K.; GEERLINGS, P.; TOURWE*, D.; ROGIERS, V.; Bioorg. Med.

A new cis-peptide bond mimetic, c~-benzyl-o-aminomethylphenylacetic acid, was synthesized and incorporated in a homodetic somatostatin analogue. Biological binding tests and 2D NMR conformational analysis indicate that the configuration of the bridge-unit asymmetric center and the orientation of the benzyl side chain play a key role in the biological activity of this type of somatostatin analogues.

SummaryIn a previous communication we reported the racemic synthesis of the cis peptide bond mimic ot-benzyl-o-

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