Synthesis, characterization and biological evaluation of cyclomontanin D.

Abstract


Rajiv Dahiya * and Hemendra Gautam

In present study, it was of interest to synthesize a natural proline-rich cyclooligopeptide - cyclomontanin D 8 by coupling of tripeptide Boc-L-Asn(bzh)-L-Pro-Gly-OH and tetrapeptide L-Leu-L-Pro-L-Tyr-L-Ala-OMe followed by cyclization of linear polypeptide fragment. Structure of synthesized cyclopeptide was confirmed by detailed spectral analysis including FTIR, 1H NMR, 13C NMR, ESIMS/MS and elemental analysis. From the results of biological evaluation, it was concluded that newly synthesized cyclooligopeptide possessed good bioactivity against Gramnegative bacteria Klebsiella pneumonia, Pseudomonas aeruginosa as well as potent antidermatophyte activity against Microsporum audouinii and Trichophyton mentagrophytes, in comparison to reference drugs - ciprofloxacin and griseofulvin. Moreover, 8 exhibited moderate antifungal activity against pathogenic Candida albicans with minimum inhibitory concentration (MIC) value of 6 g/ml.

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