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

Abstract：

:Tetrapeptides derived from glycine and beta-alanine were hooked at the C-3beta 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 microg/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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Bavikar SN,Salunke DB,Hazra BG,Pore VS,Dodd RH,Thierry J,Shirazi F,Deshpande MV,Kadreppa S,Chattopadhyay S

doi

10.1016/j.bmcl.2008.09.013

subject

Has Abstract

pub_date

2008-10-15 00:00:00

pages

5512-7

issue

20

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)01075-5

journal_volume

18

pub_type

杂志文章

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