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

• . aeruginosa quorum quenching assays was observed [56]. This highlights a notable issue when addressing intracellular targets of this Gram-negative bacterium, as permeating the outer and inner membrane while escaping efflux and enzymatic deactivation may represent a true challenge. The elucidation of the

• pocket next to T265. This also indicates that the quorum quenching activity of 36 depends on slight conformational changes. The L1 loop main chain and a rotation of the T265 side chain are hypothesized to be important for antagonistic/inverse agonistic functionality of PqsR-targeting QSIs. More recently

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

• significantly reduced. In some cases, however, resistance has already been observed (e.g., through increased expression of efflux pumps to circumvent quorum quenching), with the likelihood of the appearance of resistance mechanisms seemingly dependent upon the importance of the targeted virulence factor to the