Design, Synthesis and Biological Evaluation of Conjugates of 3-IO/I-Descladinose-azithromycin and Nucleobases against rRNA A2058G- or A2059G-Mutated Strains
Structurally unrelated antibiotics MLS[sub.B] (macrolide-lincosamide-streptogramin B) compromised with clinically resistant pathogens because of the cross-resistance resulting from the structural modification of rRNA A2058. The structure–activity relationships of a novel 3-O-descladinose azithromyci...
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| Veröffentlicht in: | Molecules (Basel, Switzerland) Switzerland), 2023-01, Vol.28 (3) |
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| container_title | Molecules (Basel, Switzerland) |
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| creator | Lian, Xiaotian Liu, Wentian Fan, Bingzhi Yu, Mingjia Liang, Jianhua |
| description | Structurally unrelated antibiotics MLS[sub.B] (macrolide-lincosamide-streptogramin B) compromised with clinically resistant pathogens because of the cross-resistance resulting from the structural modification of rRNA A2058. The structure–activity relationships of a novel 3-O-descladinose azithromycin chemotype conjugating with nucleobases were fully explored with the aid of engineered E. coli SQ110DTC and SQ110LPTD. The conjugates of macrolides with nucleobases, especially adenine, displayed antibacterial superiority over telithromycin, azithromycin and clindamycin against rRNA A2058/2059-mutated engineered E. coli strains at the cost of lowering permeability and increasing vulnerability to efflux proteins against clinical isolates. |
| doi_str_mv | 10.3390/molecules28031327 |
| format | Article |
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The conjugates of macrolides with nucleobases, especially adenine, displayed antibacterial superiority over telithromycin, azithromycin and clindamycin against rRNA A2058/2059-mutated engineered E. coli strains at the cost of lowering permeability and increasing vulnerability to efflux proteins against clinical isolates.</description><subject>Analysis</subject><subject>Azithromycin</subject><subject>Cross infection</subject><subject>Dosage and administration</subject><subject>Drug resistance in microorganisms</subject><subject>Drug therapy</subject><subject>Nosocomial infections</subject><subject>Patient outcomes</subject><subject>Prevention</subject><subject>Protein biosynthesis</subject><issn>1420-3049</issn><issn>1420-3049</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2023</creationdate><recordtype>article</recordtype><sourceid/><recordid>eNptjU1OwzAQhSMEEqVwAHaW2OLWP0mTLEMppVJpJdp9NXHs1JVjS3GCVM7CYXELCxZoFvNm5r1vouiekhHnORk3zkjRG-lZRjjlLL2IBjRmBHMS55d_9HV04_2BEEZjmgyir2fpdW0f0eZou33QHoGt0JN2xtVagEGzDzA9dNpZ5BSaOnvoa-ikP00cL9bjBQ4MYaDS1nmJ4VN3-9Y1R6HtmbXqhZGuBB8yUIO2vkPt-6pABSNJNsfItWeZz_Fb3wV0hTZde_LdRlcKjJd3v30YbV9m2-krXq7ni2mxxPUkJbiUJElYJjPJgOZKgkwEUURkRFQ8Fnmp8qzKaRqXpJSKQqkIQDgIOqEVTAQfRg8_2BqM3GmrXHgvGu3FrkhjzihllATX6B9XqEo2WjgrlQ77P4Fvfo18Vg</recordid><startdate>20230101</startdate><enddate>20230101</enddate><creator>Lian, Xiaotian</creator><creator>Liu, Wentian</creator><creator>Fan, Bingzhi</creator><creator>Yu, Mingjia</creator><creator>Liang, Jianhua</creator><general>MDPI AG</general><scope/></search><sort><creationdate>20230101</creationdate><title>Design, Synthesis and Biological Evaluation of Conjugates of 3-IO/I-Descladinose-azithromycin and Nucleobases against rRNA A2058G- or A2059G-Mutated Strains</title><author>Lian, Xiaotian ; Liu, Wentian ; Fan, Bingzhi ; Yu, Mingjia ; Liang, Jianhua</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-g670-be05528e8e2a19feae5c0f0c80cd34c9bf98d9174b0bef1abf0aa34cc161da6c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2023</creationdate><topic>Analysis</topic><topic>Azithromycin</topic><topic>Cross infection</topic><topic>Dosage and administration</topic><topic>Drug resistance in microorganisms</topic><topic>Drug therapy</topic><topic>Nosocomial infections</topic><topic>Patient outcomes</topic><topic>Prevention</topic><topic>Protein biosynthesis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Lian, Xiaotian</creatorcontrib><creatorcontrib>Liu, Wentian</creatorcontrib><creatorcontrib>Fan, Bingzhi</creatorcontrib><creatorcontrib>Yu, Mingjia</creatorcontrib><creatorcontrib>Liang, Jianhua</creatorcontrib><jtitle>Molecules (Basel, Switzerland)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Lian, Xiaotian</au><au>Liu, Wentian</au><au>Fan, Bingzhi</au><au>Yu, Mingjia</au><au>Liang, Jianhua</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Design, Synthesis and Biological Evaluation of Conjugates of 3-IO/I-Descladinose-azithromycin and Nucleobases against rRNA A2058G- or A2059G-Mutated Strains</atitle><jtitle>Molecules (Basel, Switzerland)</jtitle><date>2023-01-01</date><risdate>2023</risdate><volume>28</volume><issue>3</issue><issn>1420-3049</issn><eissn>1420-3049</eissn><abstract>Structurally unrelated antibiotics MLS[sub.B] (macrolide-lincosamide-streptogramin B) compromised with clinically resistant pathogens because of the cross-resistance resulting from the structural modification of rRNA A2058. 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| source | DOAJ Directory of Open Access Journals; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; MDPI - Multidisciplinary Digital Publishing Institute; PubMed Central; Free Full-Text Journals in Chemistry |
| subjects | Analysis Azithromycin Cross infection Dosage and administration Drug resistance in microorganisms Drug therapy Nosocomial infections Patient outcomes Prevention Protein biosynthesis |
| title | Design, Synthesis and Biological Evaluation of Conjugates of 3-IO/I-Descladinose-azithromycin and Nucleobases against rRNA A2058G- or A2059G-Mutated Strains |
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