IN VITRO AND IN VIVO ANTIBACTERIAL ACTIVITY OF KY-109, A NEW ORALLY ACTIVE CEPHALOSPORIN
The in vitro and in vivo antimicrobial potencies of KY-109, a pro-drug of KY-087, were compared with those of amoxicillin, cephalexin (CEX), and cefaclor (CCL). The following results were obtained. KY-087, which is the active form of KY-109, had broad antimicrobial spectrum against Gram-positive and...
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| Veröffentlicht in: | Journal of antibiotics 1988/07/25, Vol.41(7), pp.949-958 |
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| container_title | Journal of antibiotics |
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| creator | OBANA, YOSHIKI HASHIZUME, HIROYUKI YOSHIMI, AKIHISA NISHINO, TAKESHI |
| description | The in vitro and in vivo antimicrobial potencies of KY-109, a pro-drug of KY-087, were compared with those of amoxicillin, cephalexin (CEX), and cefaclor (CCL). The following results were obtained. KY-087, which is the active form of KY-109, had broad antimicrobial spectrum against Gram-positive and Gram-negative organisms, but showed low antimicrobial activity against Enterobacter sp., Serratia, and Pseudomonas sp. The antimicrobial activities of KY-087 against clinically isolated Gram-positive organisms were superior to those of CEX and CCL. The antimicrobial activities of KY-087 against Gram-negative organisms, such as Enterobacter sp., Serratia, and Pseudomonas sp., were less active. KY-087 showed dose-related bactericidal activity against Staphylococcus aureus and Escherichia coli. The therapeutic efficacy of KY109 against experimental intraperitoneal infections caused by Gram-positive and Gramnegative organisms in mice was comparable to that of CEX but inferior to that of CCL. In experimental granuloma pouch models in rats and kidney infection in rabbits, therapeutic efficacy of KY-109 was either comparable or superior to that of CEX and CCL. |
| doi_str_mv | 10.7164/antibiotics.41.949 |
| format | Article |
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The following results were obtained. KY-087, which is the active form of KY-109, had broad antimicrobial spectrum against Gram-positive and Gram-negative organisms, but showed low antimicrobial activity against Enterobacter sp., Serratia, and Pseudomonas sp. The antimicrobial activities of KY-087 against clinically isolated Gram-positive organisms were superior to those of CEX and CCL. The antimicrobial activities of KY-087 against Gram-negative organisms, such as Enterobacter sp., Serratia, and Pseudomonas sp., were less active. KY-087 showed dose-related bactericidal activity against Staphylococcus aureus and Escherichia coli. The therapeutic efficacy of KY109 against experimental intraperitoneal infections caused by Gram-positive and Gramnegative organisms in mice was comparable to that of CEX but inferior to that of CCL. In experimental granuloma pouch models in rats and kidney infection in rabbits, therapeutic efficacy of KY-109 was either comparable or superior to that of CEX and CCL.</description><identifier>ISSN: 0021-8820</identifier><identifier>EISSN: 1881-1469</identifier><identifier>DOI: 10.7164/antibiotics.41.949</identifier><identifier>PMID: 3417567</identifier><identifier>CODEN: JANTAJ</identifier><language>eng</language><publisher>Tokyo: JAPAN ANTIBIOTICS RESEARCH ASSOCIATION</publisher><subject>Administration, Oral ; Animals ; Antibacterial agents ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Bacterial Infections - drug therapy ; Biological and medical sciences ; Cephalosporins - pharmacology ; Male ; Medical sciences ; Mice ; Microbial Sensitivity Tests ; Pharmacology. Drug treatments ; Rabbits ; Rats ; Rats, Inbred Strains ; Urinary Tract Infections - drug therapy</subject><ispartof>The Journal of Antibiotics, 1988/07/25, Vol.41(7), pp.949-958</ispartof><rights>Japan Antibiotics Research Association</rights><rights>1988 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c5529-fd14eaa7b4374b25e4b0903cdc379aceec1a02d7012e220baea5ce1ee1b589533</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,777,781,1877,4010,27904,27905,27906</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=7812352$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3417567$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>OBANA, YOSHIKI</creatorcontrib><creatorcontrib>HASHIZUME, HIROYUKI</creatorcontrib><creatorcontrib>YOSHIMI, AKIHISA</creatorcontrib><creatorcontrib>NISHINO, TAKESHI</creatorcontrib><title>IN VITRO AND IN VIVO ANTIBACTERIAL ACTIVITY OF KY-109, A NEW ORALLY ACTIVE CEPHALOSPORIN</title><title>Journal of antibiotics</title><addtitle>J. Antibiot.</addtitle><description>The in vitro and in vivo antimicrobial potencies of KY-109, a pro-drug of KY-087, were compared with those of amoxicillin, cephalexin (CEX), and cefaclor (CCL). The following results were obtained. KY-087, which is the active form of KY-109, had broad antimicrobial spectrum against Gram-positive and Gram-negative organisms, but showed low antimicrobial activity against Enterobacter sp., Serratia, and Pseudomonas sp. The antimicrobial activities of KY-087 against clinically isolated Gram-positive organisms were superior to those of CEX and CCL. The antimicrobial activities of KY-087 against Gram-negative organisms, such as Enterobacter sp., Serratia, and Pseudomonas sp., were less active. KY-087 showed dose-related bactericidal activity against Staphylococcus aureus and Escherichia coli. The therapeutic efficacy of KY109 against experimental intraperitoneal infections caused by Gram-positive and Gramnegative organisms in mice was comparable to that of CEX but inferior to that of CCL. In experimental granuloma pouch models in rats and kidney infection in rabbits, therapeutic efficacy of KY-109 was either comparable or superior to that of CEX and CCL.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Antibacterial agents</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Bacterial Infections - drug therapy</subject><subject>Biological and medical sciences</subject><subject>Cephalosporins - pharmacology</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Microbial Sensitivity Tests</subject><subject>Pharmacology. Drug treatments</subject><subject>Rabbits</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Urinary Tract Infections - drug therapy</subject><issn>0021-8820</issn><issn>1881-1469</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1988</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE9v00AQxVcVVQmlXwAJaQ-IEw47-8e7e3SDS61acRVCISdrvZmAKycp3uTAt2dTR1FvXGZm9X4zb_UIeQdsrCGVn91m1zbtdtf6MJYwttKekREYAwnI1L4iI8Y4JMZw9pq8CeGRMaGFNhfkQkjQKtUj8rOY0odiPqtoNv1Cnx8Ph3leXGeTeT4rspLGoYjMglY39G6RALOfaEan-Q9azbKyXAxATif5_W1WVt_uq1kxfUvOV64LeHXsl-T7TT6f3CZl9bWYZGXileI2WS1BonO6kULLhiuUDbNM-KUX2jqP6MExvtQMOHLOGodOeQREaJSxSohL8nG4-9Rv_-wx7Op1Gzx2ndvgdh9qbSTTzNr_gqCApQAygnwAfb8NocdV_dS3a9f_rYHVh9zrF7nXEuqYe1x6f7y-b9a4PK0cg476h6Pugnfdqncb34YTpg1woXjE7gbsMezcLzzpro9mHb50Bpuag7seSvzEifK_XV_jRvwDIaKhHA</recordid><startdate>1988</startdate><enddate>1988</enddate><creator>OBANA, YOSHIKI</creator><creator>HASHIZUME, HIROYUKI</creator><creator>YOSHIMI, AKIHISA</creator><creator>NISHINO, TAKESHI</creator><general>JAPAN ANTIBIOTICS RESEARCH ASSOCIATION</general><general>Japan Antibiotics Research Association</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7T7</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>1988</creationdate><title>IN VITRO AND IN VIVO ANTIBACTERIAL ACTIVITY OF KY-109, A NEW ORALLY ACTIVE CEPHALOSPORIN</title><author>OBANA, YOSHIKI ; HASHIZUME, HIROYUKI ; YOSHIMI, AKIHISA ; NISHINO, TAKESHI</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5529-fd14eaa7b4374b25e4b0903cdc379aceec1a02d7012e220baea5ce1ee1b589533</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1988</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Antibacterial agents</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Bacterial Infections - drug therapy</topic><topic>Biological and medical sciences</topic><topic>Cephalosporins - pharmacology</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Microbial Sensitivity Tests</topic><topic>Pharmacology. Drug treatments</topic><topic>Rabbits</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Urinary Tract Infections - drug therapy</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>OBANA, YOSHIKI</creatorcontrib><creatorcontrib>HASHIZUME, HIROYUKI</creatorcontrib><creatorcontrib>YOSHIMI, AKIHISA</creatorcontrib><creatorcontrib>NISHINO, TAKESHI</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Industrial and Applied Microbiology Abstracts (Microbiology A)</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of antibiotics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>OBANA, YOSHIKI</au><au>HASHIZUME, HIROYUKI</au><au>YOSHIMI, AKIHISA</au><au>NISHINO, TAKESHI</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>IN VITRO AND IN VIVO ANTIBACTERIAL ACTIVITY OF KY-109, A NEW ORALLY ACTIVE CEPHALOSPORIN</atitle><jtitle>Journal of antibiotics</jtitle><addtitle>J. Antibiot.</addtitle><date>1988</date><risdate>1988</risdate><volume>41</volume><issue>7</issue><spage>949</spage><epage>958</epage><pages>949-958</pages><issn>0021-8820</issn><eissn>1881-1469</eissn><coden>JANTAJ</coden><abstract>The in vitro and in vivo antimicrobial potencies of KY-109, a pro-drug of KY-087, were compared with those of amoxicillin, cephalexin (CEX), and cefaclor (CCL). The following results were obtained. KY-087, which is the active form of KY-109, had broad antimicrobial spectrum against Gram-positive and Gram-negative organisms, but showed low antimicrobial activity against Enterobacter sp., Serratia, and Pseudomonas sp. The antimicrobial activities of KY-087 against clinically isolated Gram-positive organisms were superior to those of CEX and CCL. The antimicrobial activities of KY-087 against Gram-negative organisms, such as Enterobacter sp., Serratia, and Pseudomonas sp., were less active. KY-087 showed dose-related bactericidal activity against Staphylococcus aureus and Escherichia coli. The therapeutic efficacy of KY109 against experimental intraperitoneal infections caused by Gram-positive and Gramnegative organisms in mice was comparable to that of CEX but inferior to that of CCL. In experimental granuloma pouch models in rats and kidney infection in rabbits, therapeutic efficacy of KY-109 was either comparable or superior to that of CEX and CCL.</abstract><cop>Tokyo</cop><pub>JAPAN ANTIBIOTICS RESEARCH ASSOCIATION</pub><pmid>3417567</pmid><doi>10.7164/antibiotics.41.949</doi><tpages>10</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | The Journal of Antibiotics, 1988/07/25, Vol.41(7), pp.949-958 |
| issn | 0021-8820 1881-1469 |
| language | eng |
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| source | MEDLINE; J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese |
| subjects | Administration, Oral Animals Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Bacterial Infections - drug therapy Biological and medical sciences Cephalosporins - pharmacology Male Medical sciences Mice Microbial Sensitivity Tests Pharmacology. Drug treatments Rabbits Rats Rats, Inbred Strains Urinary Tract Infections - drug therapy |
| title | IN VITRO AND IN VIVO ANTIBACTERIAL ACTIVITY OF KY-109, A NEW ORALLY ACTIVE CEPHALOSPORIN |
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