Bioorganic and Medicinal Chemistry Letters p. 5512 - 5517 (2008)
Update date:2022-08-10
Topics:
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
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.
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Doi:10.1021/om00031a061
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