Anti-MRSA cephems. Part 3: Additional C-7 acid derivatives
Twenty-seven novel cephalosporin derivatives with activity against methicillin-resistant Staphylococcus aureus (MRSA) are described. The compounds contain novel acid moieties at C-7 that were synthesized using nucleophilic aromatic substitution reactions and Stille couplings. The most interesting co...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2003-01, Vol.11 (2), p.281-291 |
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| container_title | Bioorganic & medicinal chemistry |
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| creator | Springer, Dane M Luh, Bing-Yu Goodrich, Jason T Bronson, Joanne J |
| description | Twenty-seven novel cephalosporin derivatives with activity against methicillin-resistant
Staphylococcus aureus (MRSA) are described. The compounds contain novel acid moieties at C-7 that were synthesized using nucleophilic aromatic substitution reactions and Stille couplings. The most interesting compound (
6) displayed an MIC
90 against MRSA of 3.7 μg/mL, and an average PD
50 of 3.9 mg/kg.
Novel C-7 acid cephalosporin derivatives with good activity against methicillin-resistant
Staphylococcus aureus (MRSA) are described. The most interesting compound (
6) displayed an MIC
90 against MRSA of 3.7 μg/mL, and an average PD
50 of 3.9 mg/kg.. |
| doi_str_mv | 10.1016/S0968-0896(02)00335-8 |
| format | Article |
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Staphylococcus aureus (MRSA) are described. The compounds contain novel acid moieties at C-7 that were synthesized using nucleophilic aromatic substitution reactions and Stille couplings. The most interesting compound (
6) displayed an MIC
90 against MRSA of 3.7 μg/mL, and an average PD
50 of 3.9 mg/kg.
Novel C-7 acid cephalosporin derivatives with good activity against methicillin-resistant
Staphylococcus aureus (MRSA) are described. The most interesting compound (
6) displayed an MIC
90 against MRSA of 3.7 μg/mL, and an average PD
50 of 3.9 mg/kg..</description><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/S0968-0896(02)00335-8</identifier><identifier>PMID: 12470721</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Animals ; Anti-Bacterial Agents - chemistry ; Anti-Bacterial Agents - pharmacology ; Antibacterial agents ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Biological and medical sciences ; Cephalosporins - chemistry ; Cephalosporins - pharmacology ; Disease Models, Animal ; Lethal Dose 50 ; Medical sciences ; Methicillin Resistance ; Mice ; Microbial Sensitivity Tests ; Pharmacology. Drug treatments ; Staphylococcal Infections - microbiology ; Staphylococcus aureus - drug effects ; Staphylococcus aureus - pathogenicity ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry, 2003-01, Vol.11 (2), p.281-291</ispartof><rights>2002 Elsevier Science Ltd</rights><rights>2003 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0968-0896(02)00335-8$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,781,785,3551,27926,27927,45997</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=14043022$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12470721$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Springer, Dane M</creatorcontrib><creatorcontrib>Luh, Bing-Yu</creatorcontrib><creatorcontrib>Goodrich, Jason T</creatorcontrib><creatorcontrib>Bronson, Joanne J</creatorcontrib><title>Anti-MRSA cephems. Part 3: Additional C-7 acid derivatives</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem</addtitle><description>Twenty-seven novel cephalosporin derivatives with activity against methicillin-resistant
Staphylococcus aureus (MRSA) are described. The compounds contain novel acid moieties at C-7 that were synthesized using nucleophilic aromatic substitution reactions and Stille couplings. The most interesting compound (
6) displayed an MIC
90 against MRSA of 3.7 μg/mL, and an average PD
50 of 3.9 mg/kg.
Novel C-7 acid cephalosporin derivatives with good activity against methicillin-resistant
Staphylococcus aureus (MRSA) are described. The most interesting compound (
6) displayed an MIC
90 against MRSA of 3.7 μg/mL, and an average PD
50 of 3.9 mg/kg..</description><subject>Animals</subject><subject>Anti-Bacterial Agents - chemistry</subject><subject>Anti-Bacterial Agents - pharmacology</subject><subject>Antibacterial agents</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Biological and medical sciences</subject><subject>Cephalosporins - chemistry</subject><subject>Cephalosporins - pharmacology</subject><subject>Disease Models, Animal</subject><subject>Lethal Dose 50</subject><subject>Medical sciences</subject><subject>Methicillin Resistance</subject><subject>Mice</subject><subject>Microbial Sensitivity Tests</subject><subject>Pharmacology. Drug treatments</subject><subject>Staphylococcal Infections - microbiology</subject><subject>Staphylococcus aureus - drug effects</subject><subject>Staphylococcus aureus - pathogenicity</subject><subject>Structure-Activity Relationship</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpF0EtLAzEQwPEgiq3Vj6DsRdBD6uS1m_RSluILKorVc0iTWYy027JZC357-1JPc_kxzPwJOWfQZ8DymwmYXFPQJr8Cfg0ghKL6gHSZzCUVwrBD0v0jHXKS0icAcGnYMekwLgsoOOuSQVm3kT69TsrM4_ID56mfvbimzcQgK0OIbVzUbpaNaJE5H0MWsIkr18YVplNyVLlZwrP97JH3u9u30QMdP98_jsoxRW5ES7nTYcqc1M4JZpTQjgmHgeUMuWSKF0JOjSpMVelKISr0QeiqUMCDNJgr0SMXu73Lr-kcg102ce6ab_v7xBpc7oFL3s2qxtU-pn8nQQrgfO2GO4fra1cRG5t8xNpjiA361oZFtAzsJq_d5rWbdha43ea1WvwAZTloIw</recordid><startdate>20030117</startdate><enddate>20030117</enddate><creator>Springer, Dane M</creator><creator>Luh, Bing-Yu</creator><creator>Goodrich, Jason T</creator><creator>Bronson, Joanne J</creator><general>Elsevier Ltd</general><general>Elsevier Science</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope></search><sort><creationdate>20030117</creationdate><title>Anti-MRSA cephems. Part 3: Additional C-7 acid derivatives</title><author>Springer, Dane M ; Luh, Bing-Yu ; Goodrich, Jason T ; Bronson, Joanne J</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-e293t-2a8db1a48aa319538a13aed161e24152734b9579ff8f5ee5ecd38f7502d49e653</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2003</creationdate><topic>Animals</topic><topic>Anti-Bacterial Agents - chemistry</topic><topic>Anti-Bacterial Agents - pharmacology</topic><topic>Antibacterial agents</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Biological and medical sciences</topic><topic>Cephalosporins - chemistry</topic><topic>Cephalosporins - pharmacology</topic><topic>Disease Models, Animal</topic><topic>Lethal Dose 50</topic><topic>Medical sciences</topic><topic>Methicillin Resistance</topic><topic>Mice</topic><topic>Microbial Sensitivity Tests</topic><topic>Pharmacology. Drug treatments</topic><topic>Staphylococcal Infections - microbiology</topic><topic>Staphylococcus aureus - drug effects</topic><topic>Staphylococcus aureus - pathogenicity</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Springer, Dane M</creatorcontrib><creatorcontrib>Luh, Bing-Yu</creatorcontrib><creatorcontrib>Goodrich, Jason T</creatorcontrib><creatorcontrib>Bronson, Joanne J</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Springer, Dane M</au><au>Luh, Bing-Yu</au><au>Goodrich, Jason T</au><au>Bronson, Joanne J</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Anti-MRSA cephems. Part 3: Additional C-7 acid derivatives</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem</addtitle><date>2003-01-17</date><risdate>2003</risdate><volume>11</volume><issue>2</issue><spage>281</spage><epage>291</epage><pages>281-291</pages><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>Twenty-seven novel cephalosporin derivatives with activity against methicillin-resistant
Staphylococcus aureus (MRSA) are described. The compounds contain novel acid moieties at C-7 that were synthesized using nucleophilic aromatic substitution reactions and Stille couplings. The most interesting compound (
6) displayed an MIC
90 against MRSA of 3.7 μg/mL, and an average PD
50 of 3.9 mg/kg.
Novel C-7 acid cephalosporin derivatives with good activity against methicillin-resistant
Staphylococcus aureus (MRSA) are described. The most interesting compound (
6) displayed an MIC
90 against MRSA of 3.7 μg/mL, and an average PD
50 of 3.9 mg/kg..</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>12470721</pmid><doi>10.1016/S0968-0896(02)00335-8</doi><tpages>11</tpages></addata></record> |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Animals Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Cephalosporins - chemistry Cephalosporins - pharmacology Disease Models, Animal Lethal Dose 50 Medical sciences Methicillin Resistance Mice Microbial Sensitivity Tests Pharmacology. Drug treatments Staphylococcal Infections - microbiology Staphylococcus aureus - drug effects Staphylococcus aureus - pathogenicity Structure-Activity Relationship |
| title | Anti-MRSA cephems. Part 3: Additional C-7 acid derivatives |
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