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Synthesis of Quinazolinone Conjugated Shorter Analogues of Bactenecin7 as Potent Antimicrobials

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A series of shorter peptide analogues of Bactenecin7 (RP, PRP, GPRP and RPRP) were synthesized and conjugated to 3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanoic acid to study the effect of conjugation. All the peptides and their conjugates were characterized by analytical and spectroscopic techniques. The synthesized compounds viz., peptides, heterocyclic conjugates and the hydrogenolyzed products were evaluated for antimicrobial activity against a panel of pathogens. The results revealed that all the conjugates have shown enhanced activity than their counterparts. Further, hydrogenolyzed tetrapeptide conjugates (10 and 13) have exerted highly potent activity nearly 3-4 times than the standard drugs used.

Keywords: Quinazolinone; bactenecin7; conjugation; potent antimicrobials

Document Type: Research Article


Publication date: 2013-02-01

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  • Protein & Peptide Letters publishes short papers in all important aspects of protein and peptide research, including structural studies, recombinant expression, function, synthesis, enzymology, immunology, molecular modeling, drug design etc. Manuscripts must have a significant element of novelty, timeliness and urgency that merit rapid publication. Reports of crystallisation, and preliminary structure determinations of biologically important proteins are acceptable. Purely theoretical papers are also acceptable provided they provide new insight into the principles of protein/peptide structure and function.
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