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Mar. Drugs 2014, 12(5), 2458-2470; doi:10.3390/md12052458
Article

Marinopyrrole Derivatives as Potential Antibiotic Agents against Methicillin-Resistant Staphylococcus aureus (III)

1,2,3,†
, 4,5,†
, 5
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 and 1,2,3,6,*
Received: 10 February 2014; in revised form: 21 March 2014 / Accepted: 24 March 2014 / Published: 30 April 2014
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Abstract: The marine natural product, marinopyrrole A (1), was previously shown to have significant antibiotic activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA). Although compound (1) exhibits a significant reduction in MRSA activity in the presence of human serum, we have identified key modifications that partially restore activity. We previously reported our discovery of a chloro-derivative of marinopyrrole A (1a) featuring a 2–4 fold improved minimum inhibitory concentration (MIC) against MRSA, significantly less susceptibility to serum inhibition and rapid and concentration-dependent killing of MRSA. Here, we report a novel fluoro-derivative of marinopyrrole A (1e) showing an improved profile of potency, less susceptibility to serum inhibition, as well as rapid and concentration-dependent killing of MRSA.
Keywords: antibiotics; non-symmetrical marinopyrroles; MRSA; SAR antibiotics; non-symmetrical marinopyrroles; MRSA; SAR
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Liu, Y.; Haste, N.M.; Thienphrapa, W.; Li, J.; Nizet, V.; Hensler, M.; Li, R. Marinopyrrole Derivatives as Potential Antibiotic Agents against Methicillin-Resistant Staphylococcus aureus (III). Mar. Drugs 2014, 12, 2458-2470.

AMA Style

Liu Y, Haste NM, Thienphrapa W, Li J, Nizet V, Hensler M, Li R. Marinopyrrole Derivatives as Potential Antibiotic Agents against Methicillin-Resistant Staphylococcus aureus (III). Marine Drugs. 2014; 12(5):2458-2470.

Chicago/Turabian Style

Liu, Yan; Haste, Nina M.; Thienphrapa, Wdee; Li, Jerry; Nizet, Victor; Hensler, Mary; Li, Rongshi. 2014. "Marinopyrrole Derivatives as Potential Antibiotic Agents against Methicillin-Resistant Staphylococcus aureus (III)." Mar. Drugs 12, no. 5: 2458-2470.


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