ChemInform Abstract: Synthesis and Biological Activities of New N-Formylated Methionyl Peptides Containing an α-Substituted Glycine Residue

Autor: G. Attardo, J. L. Kraus
Rok vydání: 2010
Předmět:
Zdroj: ChemInform. 23
ISSN: 0931-7597
DOI: 10.1002/chin.199226259
Popis: Small molecular weight peptides related to the well-known chemotactic peptide N -α-formyl-methionyl-leucyl-phenylalanine have been prepared. These compounds were designed to evaluate the requirements in position 3 (phenylalanine). Each analogue containing an α-substituted glycine in position 3 was tested for its ability to induce lysosomal enzyme release from cytochalasin B treated human neutrophils. In addition, each analogue was also tested for its ability to antagonize superoxide generation. The results indicate that the analogue N -formyl-methionyl-leucyl-(α-anilino)glycine allyl ester is a potent antagonist of superoxide generation. Its ID 50 's suggest that this compound could be very promising in the field of anti-inflammatory drugs. A hypothetical inhibition mechanism is discussed.
Databáze: OpenAIRE