Working Paper Article Version 1 This version is not peer-reviewed

In Vitro and In vivo Activity of 14-O-[(4,6-Diamino-Pyrimidine-2-yl) Thioacetyl] Mutilin Against Methicillin-Resistant Staphylococcus aureus

Version 1 : Received: 9 April 2021 / Approved: 12 April 2021 / Online: 12 April 2021 (12:18:08 CEST)

A peer-reviewed article of this Preprint also exists.

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. 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.

Journal reference: Molecules 2021, 26, 3277
DOI: 10.3390/molecules26113277

Abstract

Staphylococcus aureus (S. aureus) is a major human pathogen that requires new antibiotics with unique mechanism. A new pleuromutilin derivative, 14-O-[(4,6-Diaminopyrimidine-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.

Keywords

DPTM; Methicillin-resistant Staphylococcus aureus (MRSA); Antibacterial activity; Murine skin wound model; MIC

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