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In Vitro and In Vivo Activity of 14-O-[(4,6-Diamino-pyrimidine-2-yl) thioacetyl] Mutilin against Methicillin-Resistant Staphylococcus aureus

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Zhengzhou Key Laboratory of Immunopharmacology of Effective Components of Chinese Veterinary Medicine, College of Veterinary Medicine, Henan University of Animal Husbandry and Economy, Zhengzhou 450046, China
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Henan Provincial Research Center for the Inheritance and Innovation of Chinese Veterinary Medicine Classic Prescriptions, College of Veterinary Medicine, Henan University of Animal Husbandry and Economy, Zhengzhou 450046, China
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Department of Animal Production, Jinhua Polytechnic, Jinhua 321000, China
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Key Laboratory of Veterinary Pharmaceutical Development, Ministry of Agriculture and Rural Affairs, Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, Lanzhou 730050, China
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Authors to whom correspondence should be addressed.
Academic Editor: Jean-Marc Sabatier
Molecules 2021, 26(11), 3277; https://doi.org/10.3390/molecules26113277
Received: 6 April 2021 / Revised: 13 May 2021 / Accepted: 20 May 2021 / Published: 28 May 2021
Staphylococcus aureus (S. aureus) is a major human pathogen that requires new antibiotics with unique mechanism. A new pleuromutilin derivative, 14-O-[(4,6-Diamino-pyrimidine-2-yl) thioacetyl] mutilin (DPTM), has been synthesized and proved as a potent antibacterial agent using in vitro and in vivo assays. In the present study, DPTM was further in vitro evaluated against methicillin-resistant Staphylococcus aureus (MRSA) isolated from dairy farms and outperformed tiamulin fumarate, a pleuromutilin drug used for veterinary. Moreover, a murine skin wound model caused by MRSA infection was established, and the healing effect of DPTM was investigated. The results showed that DPTM could promote the healing of MRSA skin infection, reduce the bacterial burden of infected skin MRSA and decrease the secretion of IL-6 and TNF-α inflammatory cytokines in plasma. These results provided the basis for further in-depth drug targeted studies of DPTM as a novel antibacterial agent. View Full-Text
Keywords: DPTM; methicillin-resistant Staphylococcus aureus (MRSA); antibacterial activity; murine skin wound model; MIC DPTM; methicillin-resistant Staphylococcus aureus (MRSA); antibacterial activity; murine skin wound model; MIC
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MDPI and ACS Style

Fu, Y.; Leng, C.; Fan, Y.; Ma, X.; Li, X.; Wang, X.; Guo, Z.; Wang, X.; Shang, R. In Vitro and In Vivo Activity of 14-O-[(4,6-Diamino-pyrimidine-2-yl) thioacetyl] Mutilin against Methicillin-Resistant Staphylococcus aureus. Molecules 2021, 26, 3277. https://doi.org/10.3390/molecules26113277

AMA Style

Fu Y, Leng C, Fan Y, Ma X, Li X, Wang X, Guo Z, Wang X, Shang R. In Vitro and In Vivo Activity of 14-O-[(4,6-Diamino-pyrimidine-2-yl) thioacetyl] Mutilin against Methicillin-Resistant Staphylococcus aureus. Molecules. 2021; 26(11):3277. https://doi.org/10.3390/molecules26113277

Chicago/Turabian Style

Fu, Yunxing, Chunqing Leng, Yuan Fan, Xia Ma, Xianghui Li, Xuefei Wang, Zhenghuan Guo, Xiujun Wang, and Ruofeng Shang. 2021. "In Vitro and In Vivo Activity of 14-O-[(4,6-Diamino-pyrimidine-2-yl) thioacetyl] Mutilin against Methicillin-Resistant Staphylococcus aureus" Molecules 26, no. 11: 3277. https://doi.org/10.3390/molecules26113277

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