Based on modeling studies, we hypothesized that tylosin derivatives without formyl group should rather adopt an erythromycin-like binding mode to the ribosome. Twenty four 16-membered macrocyclic compounds were accessed by multicomponent reactions (Gewald, Ugi) of tylosin and investigated for their antituberculosis activity. The best compound was twice as active as tylosin and might thus be a good starting point for further optimization of biological properties.

Tylosin derivatives (III) and (VII) are synthesized by Gewald or Ugi three-component reaction, resp., and evaluated for their antituberculosis activities. Compound (IIIe) is slightly better than tylosin itself. Structure-activity relationship is discussed. -(KIM, D.; HUANG, Y.; WANG, K.; DOEMLING*, A.; Chem. Heterocycl. Compd. (N. Y., NY, U. S.) 49 (2013) 6, 849-859, http://dx.

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