A solid-phase method for the synthesis of 1,2,3, 4-tetrahydro-beta-carboline-containing peptidomimetics has been developed. The key step in the strategy is the Pictet-Spengler condensation of a resin-bound tryptophan-containing fragment with an Fmoc-amino aldehyde.

background: the rise of opportunistic fungal infections highlights the need for development of new antimicrobial agents. antimicrobial peptides (amps) and antifungal peptides (afps) are among the agents with minimal resistance being developed against them, therefore they can be used as structural templates for design of new antimicrobial agents. methods: in the present study four antifungal pep...

A novel selectively sequential C-S/C-N bond activation is presented. Through the combination of an Ugi-4CR and cleavage, diverse peptidomimetics containing a primary amide are prepared in a...

A Ni-catalyzed reductive carboxylation of N-substituted aziridines with CO2 at atmospheric pressure is disclosed. The protocol characterized by its mild conditions, experimental ease, and exquisite chemo- regioselectivity pattern, thus unlocking a new catalytic blueprint to access ?-amino acids, important building blocks considerable potential as peptidomimetics.

Biologics such as monoclonal antibodies (mAb) and soluble receptors represent new classes of therapeutic agents for treatment of several diseases. High affinity and high specificity biologics can be utilized for variety of clinical purposes. Monoclonal antibodies have been used as diagnostic agents when coupled with radionuclide, immune modulatory agents or in the treatment of cancers. Among ot...

The design of novel chemoselective and site-specific ligation methods provides new tools for obtaining complex scaffolds, peptidomimetics, and peptide conjugates. The chemistry of the N-phenylthiocarbonyl group has led to several developments in peptide ligation chemistry and peptide bioconjugation during the last 10 years. The aim of this review is to provide an overview of this emerging field.