International Journal of Anatomy and Physiology

ISSN 2326-7275

International Journal of Anatomy and Physiology ISSN: 2326-7275 Vol. 6 (11), pp. 001-007, November, 2017. © International Scholars Journals

Full Length Research Paper

Synthesis, characterization and biological evaluation of cyclomontanin D

Rajiv Dahiya1* and Hemendra Gautam2

1Department of Pharmaceutical Chemistry, Globus College of Pharmacy, Bhojpur Road, Bhopal 462 045, Madhya Pradesh, India.

2Department of Pharmaceutical Chemistry, NRI Institute of Pharmacy, Raisen Road, Bhopal 462 021, Madhya Pradesh, India.

Accepted 25 March, 2017

Abstract

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 Gram-negative 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 mg/ml.

Key words: Annona montana, cyclomontanin D, cyclic heptapeptide, peptide synthesis, antibacterial activity, antidermatophyte activity.