Abstract
Elastin protein-based polymers have their origin in repeating sequences of the mammalian elastic protein, elastin. The sequences of elastin peptides chosen are tetrapeptides, pentapeptides and tricosamers (30 amino acids) and also aromatic amino acids. These have been conjugated to 1-(2,3-dichlorophenyl)piperazine to study the effect of conjugation on the activity. The conjugates so obtained were characterized by physical and analytical techniques followed by the antimicrobial evaluation. The study revealed that all the conjugates have exhibited enhanced activity than the conventional drugs. Further, the conjugates of tricosamers have shown extraordinary activity against the fungal species with MIC value of 3–5 μg/ml which is five fold more potent than the antibiotic used.
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Abbreviations
- Boc:
-
t-Butoxycarbonyl
- EDCI:
-
1-(3-Dimethylaminopropyl)-3-ethyl-carbodiimide.HCl
- HOBt:
-
1-Hydroxybenzotriazole
- IBCF:
-
Isobutyl chloroformate
- NMM:
-
N-methyl morpholine
- TFA:
-
Trifluoroacetic acid
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One of the authors RS gratefully acknowledges Lady Tata Memorial Trust, Mumbai for the award of Junior Research Scholarship.
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Suhas, R., Chandrashekar, S. & Gowda, D.C. A New Family of Highly Potent Inhibitors of Microbes: Synthesis and Conjugation of Elastin Based Peptides to Piperazine Derivative. Int J Pept Res Ther 18, 89–98 (2012). https://doi.org/10.1007/s10989-011-9282-8
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DOI: https://doi.org/10.1007/s10989-011-9282-8