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We evaluated the in\u2010vitro antibacterial activities of the derivatives against methicillin\u2010resistant <jats:italic>Staphylococcus aureus<\/jats:italic> (MRSA, ATCC 43300), <jats:italic>Staphylococcus aureus<\/jats:italic> (ATCC 29213) and <jats:italic>Escherichia coli<\/jats:italic> (ATCC 25922). The majority of the synthesized derivatives possessed moderate antibacterial activities. Compound <jats:bold>8<\/jats:bold> was found to be the most active antibacterial derivative against MRSA. We conducted docking experiments to understand the possible mode of interactions between compounds <jats:bold>8<\/jats:bold>,<jats:bold> 9b<\/jats:bold>,<jats:bold> 11a<\/jats:bold> and 50S ribosomal subunit. The docking results proved that there is a reasonable correlation between the binding free energy and the antibacterial activity. Compound <jats:bold>8<\/jats:bold> was evaluated for its in\u2010vivo antibacterial activity and showed higher efficacy than tiamulin against MRSA in mouse infection model.<\/jats:p>","DOI":"10.1111\/cbdd.13328","type":"journal-article","created":{"date-parts":[[2018,5,3]],"date-time":"2018-05-03T08:52:41Z","timestamp":1525337561000},"page":"1627-1637","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":25,"title":["Synthesis and antibacterial activities of novel pleuromutilin derivatives bearing an aminothiophenol moiety"],"prefix":"10.1111","volume":"92","author":[{"given":"Zhao\u2010Sheng","family":"Zhang","sequence":"first","affiliation":[{"name":"Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation College of Veterinary Medicine South China Agricultural University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yun\u2010Zhen","family":"Huang","sequence":"additional","affiliation":[{"name":"Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation College of Veterinary Medicine South China Agricultural University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jian","family":"Luo","sequence":"additional","affiliation":[{"name":"Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation College of Veterinary Medicine South China Agricultural University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhen","family":"Jin","sequence":"additional","affiliation":[{"name":"Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation College of Veterinary Medicine South China Agricultural University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ya\u2010Hong","family":"Liu","sequence":"additional","affiliation":[{"name":"Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation College of Veterinary Medicine South China Agricultural University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-2293-0287","authenticated-orcid":false,"given":"You\u2010Zhi","family":"Tang","sequence":"additional","affiliation":[{"name":"Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation College of Veterinary Medicine South China Agricultural University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2018,5,31]]},"reference":[{"key":"e_1_2_8_2_1","doi-asserted-by":"publisher","DOI":"10.1021\/acsmedchemlett.6b00057"},{"key":"e_1_2_8_3_1","doi-asserted-by":"publisher","DOI":"10.1517\/13543780903505092"},{"key":"e_1_2_8_4_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.6b00372"},{"key":"e_1_2_8_5_1","doi-asserted-by":"publisher","DOI":"10.1093\/cid\/cir935"},{"key":"e_1_2_8_6_1","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00613-16"},{"key":"e_1_2_8_7_1","doi-asserted-by":"publisher","DOI":"10.1093\/jac\/dkv225"},{"key":"e_1_2_8_8_1","first-page":"35","volume":"9","author":"Chipolombwe J.","year":"2016","journal-title":"Infect. 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