{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,12]],"date-time":"2025-10-12T04:16:33Z","timestamp":1760242593683,"version":"build-2065373602"},"reference-count":24,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2017,12,4]],"date-time":"2017-12-04T00:00:00Z","timestamp":1512345600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>A novel series of 11,12-cyclic carbonate azithromycin-3-O-descladinosyl-3-O-carbamoyl glycosyl derivatives were designed, synthesized, and evaluated for their antibacterial activities in vitro. Most of these compounds had significant antibacterial activity against seven kinds of susceptible strains. In particular, compound G1 exhibited the most potent activity against methicillin-resistant Streptococcus pneumoniae 943 (MIC: 1 \u03bcg\/mL), Staphylococcus pneumoniae 746 (MIC: 2 \u03bcg\/mL), Streptococcus pyogenes 447 (MIC: 8 \u03bcg\/mL), and Escherichia coli 236 (MIC: 32 \u03bcg\/mL), which were two-, four-, four-, four-, and eight-fold stronger activity than azithromycin, respectively. Additionally, compound G2 exhibited improved activity against methicillin-resistant Staphylococcus aureus MRSA-1 (MIC: 8 \u03bcg\/mL), Streptococcus pneumoniae 943 (MIC: 2 \u03bcg\/mL), Staphylococcus pneumoniae 746 (MIC: 2 \u03bcg\/mL), and Escherichia coli 236 (MIC: 32 \u03bcg\/mL), which were two-, two-, four-, and eight-fold better activity than azithromycin, respectively. As for methicillin-resistant Staphylococcus aureus MRSA-1, compound G6 presented the most excellent activity (MIC: 4 \u03bcg\/mL), showing four-fold higher activity than azithromycin (MIC: 16 \u03bcg\/mL) and erythromycin (MIC: 16 \u03bcg\/mL). However, compared with other compounds, compounds G7 and G8 with the disaccharide side chain were observed the lower activity against seven strains.<\/jats:p>","DOI":"10.3390\/molecules22122146","type":"journal-article","created":{"date-parts":[[2017,12,4]],"date-time":"2017-12-04T11:16:38Z","timestamp":1512386198000},"page":"2146","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Synthesis and Antibacterial Evaluation of a Series of 11,12-Cyclic Carbonate Azithromycin-3-O-descladinosyl-3-O-carbamoyl Glycosyl Derivatives"],"prefix":"10.3390","volume":"22","author":[{"given":"Chao-Ming","family":"Wang","sequence":"first","affiliation":[{"name":"School of Pharmacy, Key Laboratory ofMolecular Pharmacology and Drug Evaluation,Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, 30 Qingquan Road, Yantai 264005, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Feng-Lan","family":"Zhao","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Key Laboratory ofMolecular Pharmacology and Drug Evaluation,Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, 30 Qingquan Road, Yantai 264005, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Lei","family":"Zhang","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Key Laboratory ofMolecular Pharmacology and Drug Evaluation,Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, 30 Qingquan Road, Yantai 264005, China"},{"name":"Department of Organic Chemistry, College of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xiao-Yun","family":"Chai","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, College of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Qing-Guo","family":"Meng","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Key Laboratory ofMolecular Pharmacology and Drug Evaluation,Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, 30 Qingquan Road, Yantai 264005, China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2017,12,4]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1101\/cshperspect.a025395","article-title":"Resistance to Macrolide Antibiotics in Public Health Pathogens","volume":"6","author":"Fyfe","year":"2016","journal-title":"Cold Spring Harb. 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