Synthesis of novel sulfide-based cyclic peptidomimetic analogues to solonamides

• José Brango-Vanegas,
• Luan A. Martinho,
• Lucinda J. Bessa,
• Andreanne G. Vasconcelos,
• Alexandra Plácido,
• Alex L. Pereira,
• José R. S. A. Leite and
• Angelo H. L. Machado

Beilstein J. Org. Chem. 2019, 15, 2544–2551, doi:10.3762/bjoc.15.247

• reported for solonamides. Keywords: antivirulence drug; bacteria; macrocyclization; pathoblocker; quorum quenching; Introduction The cyclodepsipeptides called solonamides A and B are natural molecules extracted from the marine bacterium Photobacterium halotolerans [1][2] (Figure 1). They are able to

Targeting the Pseudomonas quinolone signal quorum sensing system for the discovery of novel anti-infective pathoblockers

• Christian Schütz and
• Martin Empting

Beilstein J. Org. Chem. 2018, 14, 2627–2645, doi:10.3762/bjoc.14.241

• highlights the published drug discovery efforts providing insights into the compound binding modes if available. Furthermore, suitability of the individual targets for pathoblocker design is discussed. Keywords: anti-infectives; pathoblockers; PQS; Pseudomonas aeruginosa; quorum sensing; Introduction In

• ]. Conclusion In the past decade, the pqs QS system of P. aeruginosa has attracted increasing interest by academic researchers. This is certainly due to its prominent involvement in virulence regulation of this important Gram-negative pathogen. Among the various pathoblocker strategies, targeting a master

• the applicability of RhlR as an effective ‘stand-alone’ pathoblocker target. A combination of rhl- and pqs-targeting QSI, however, seemed to provide promising and clear-cut antivirulence effects [88]. Finally, the potential of iqs-targeting approaches remains to be investigated as more insight in the

Pathoblockers or antivirulence drugs as a new option for the treatment of bacterial infections

• Matthew B. Calvert,
• Varsha R. Jumde and
• Alexander Titz

Beilstein J. Org. Chem. 2018, 14, 2607–2617, doi:10.3762/bjoc.14.239

• pubmed.gov database yields 292 references on the topic (as of 06/08/2018), with an exponential increase over the years. Unfortunately, as the terms ‘antivirulence’ and ‘pathoblocker’ are often used interchangeably, many publications in the field are not found in this type of search, for example the

• ] which are also important for mediating bacterial virulence in vivo [33]. Therefore, both LecA and LecB have served as targets for pathoblocker development [22][23][30][34][35]. As a result of the comparatively low affinity of both lectins towards their natural carbohydrate ligands (α-galactosides for