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Mar. Drugs 2013, 11(8), 2927-2948; doi:10.3390/md11082927
Article

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

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Received: 13 June 2013; in revised form: 17 July 2013 / Accepted: 24 July 2013 / Published: 15 August 2013
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Abstract: Methicillin-resistant Staphylococcus aureus (MRSA) continues to be a major problem, causing severe and intractable infections worldwide. MRSA is resistant to all beta-lactam antibiotics, and alternative treatments are limited. A very limited number of new antibiotics have been discovered over the last half-century, novel agents for the treatment of MRSA infections are urgently needed. Marinopyrrole A was reported to show antibiotic activity against MRSA in 2008. After we reported the first total synthesis of (±)-marinopyrrole A, we designed and synthesized a series of marinopyrrole derivatives. Our structure activity relationship (SAR) studies of these novel derivatives against a panel of Gram-positive pathogens in antibacterial assays have revealed that a para-trifluoromethyl analog (33) of marinopyrrole A is ≥63-, 8-, and 4-fold more potent than vancomycin against methicillin-resistant Staphylococcus epidermidis (MRSE), methicillin-susceptible Staphylococcus aureus (MSSA) and MRSA, respectively. The results provide valuable information in the search for new-generation antibiotics.
Keywords: antibiotics; marinopyrroles; MRSA; MRSE; MSSA; SAR antibiotics; marinopyrroles; MRSA; MRSE; MSSA; 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

Cheng, C.; Liu, Y.; Song, H.; Pan, L.; Li, J.; Qin, Y.; Li, R. Marinopyrrole Derivatives as Potential Antibiotic Agents against Methicillin-Resistant Staphylococcus aureus (II). Mar. Drugs 2013, 11, 2927-2948.

AMA Style

Cheng C, Liu Y, Song H, Pan L, Li J, Qin Y, Li R. Marinopyrrole Derivatives as Potential Antibiotic Agents against Methicillin-Resistant Staphylococcus aureus (II). Marine Drugs. 2013; 11(8):2927-2948.

Chicago/Turabian Style

Cheng, Chunwei; Liu, Yan; Song, Hao; Pan, Lili; Li, Jerry; Qin, Yong; Li, Rongshi. 2013. "Marinopyrrole Derivatives as Potential Antibiotic Agents against Methicillin-Resistant Staphylococcus aureus (II)." Mar. Drugs 11, no. 8: 2927-2948.



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