Synthesis of chimeric tetrapeptide-linked cholic acid derivatives: impending synergistic agents

Bavikar, Sudhir N. ; Salunke, Deepak B. ; Hazra, Braja G. ; Pore, Vandana S. ; Dodd, Robert H. ; Thierry, Josiane ; Shirazi, Fazal ; Deshpande, Mukund V. ; Kadreppa, Sreenath ; Chattopadhyay, Samit (2008) Synthesis of chimeric tetrapeptide-linked cholic acid derivatives: impending synergistic agents Bioorganic & Medicinal Chemistry Letters, 18 (20). pp. 5512-5517. ISSN 0960-894X

Full text not available from this repository.

Official URL: http://www.sciencedirect.com/science/article/pii/S...

Related URL: http://dx.doi.org/10.1016/j.bmcl.2008.09.013

Abstract

Tetrapeptides derived from glycine and β-alanine were hooked at the C-3β position of the modified cholic acid to realize novel linear tetrapeptide-linked cholic acid derivatives. All the synthesized compounds were tested against a wide variety of microorganisms (Gram-negative bacteria, Gram-positive bacteria and fungi) and their cytotoxicity was evaluated against human embryonic kidney (HEK293) and human mammary adenocarcinoma (MCF-7) cell lines. While relatively inactive by themselves, these compounds interact synergistically with antibiotics such as fluconazole and erythromycin to inhibit growth of fungi and bacteria, respectively, at 1-24 μg/mL. The synergistic effect shown by our novel compounds is due to their inherent amphiphilicity. The fractional inhibitory concentrations reported are comparable to those reported for Polymyxin B derivatives.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:Cholic Acid; Tetrapeptide; Synergism; Antimicrobial Activity; Cytotoxicity
ID Code:60232
Deposited On:08 Sep 2011 09:34
Last Modified:08 Sep 2011 09:34

Repository Staff Only: item control page