No abstract

A microwave‐assisted solid‐phase Suzuki–Miyaura reaction has been employed for the synthesis of 5‐arylhistidine‐containing peptides. In particular, sequences containing a 5‐arylhistidine at the 1‐ or 4‐positions have been designed based on lead antimicrobial peptides. The cross‐coupling involved the arylation of a resin‐bound 5‐bromohistidine with an arylboronic acid in solution under microwave irradiation. This protocol is compatible with common protecting groups used in peptide chemistry. The resulting biaryl linear undecapeptides were screened for their antibacterial, antifungal and hemolytic activities. The results showed that the presence of an imidazole ring significantly decreases the cytotoxicity.

No abstract

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.