کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1364769 | 981545 | 2008 | 6 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis of chimeric tetrapeptide-linked cholic acid derivatives: Impending synergistic agents Synthesis of chimeric tetrapeptide-linked cholic acid derivatives: Impending synergistic agents](/preview/png/1364769.png)
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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Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 20, 15 October 2008, Pages 5512–5517