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ANTIBACTERIAL ACTIVITY OF DL 473, A NEW SEMISYNTHETIC RIFAMYCIN DERIVATIVE
DL 473, a new semisynthetic rifamycin, was 2-10 times more active in vitro than rifampicin (RAMP) against several clinical isolates of Mycobacterium tuberculosis and only slightly less active than RAMP against Gram-positive and Gram-negative bacteria. It showed excellent therapeutic activity in mice...
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Published in: | Journal of antibiotics 1981, Vol.34(8), pp.1026-1032 |
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container_end_page | 1032 |
container_issue | 8 |
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container_title | Journal of antibiotics |
container_volume | 34 |
creator | ARIOLI, VITTORIO BERTI, MARISA CARNITI, GIULIANA RANDISI, ELEONORA ROSSI, ELSA SCOTTI, ROBERTO |
description | DL 473, a new semisynthetic rifamycin, was 2-10 times more active in vitro than rifampicin (RAMP) against several clinical isolates of Mycobacterium tuberculosis and only slightly less active than RAMP against Gram-positive and Gram-negative bacteria. It showed excellent therapeutic activity in mice in experimental infections caused by Staphylococcus aureus, Streptococcus pyogenes group A, Streptococcus pneumoniae and Klebsiella pneumoniae. In the experimental TB infection in the mouse DL 473 was clearly more active than isoniazide and RAMP, two of the most effective antitubercular drugs in current use. The LD50 in the mouse was significantly higher than that of RAMP and the half-life was about 5 times longer than that of RAMP. |
doi_str_mv | 10.7164/antibiotics.34.1026 |
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It showed excellent therapeutic activity in mice in experimental infections caused by Staphylococcus aureus, Streptococcus pyogenes group A, Streptococcus pneumoniae and Klebsiella pneumoniae. In the experimental TB infection in the mouse DL 473 was clearly more active than isoniazide and RAMP, two of the most effective antitubercular drugs in current use. The LD50 in the mouse was significantly higher than that of RAMP and the half-life was about 5 times longer than that of RAMP.</description><identifier>ISSN: 0021-8820</identifier><identifier>EISSN: 1881-1469</identifier><identifier>DOI: 10.7164/antibiotics.34.1026</identifier><identifier>PMID: 7319918</identifier><language>eng</language><publisher>Japan: JAPAN ANTIBIOTICS RESEARCH ASSOCIATION</publisher><subject>Animals ; Anti-Bacterial Agents - pharmacology ; Bacteria - drug effects ; Bacterial Infections - drug therapy ; Dose-Response Relationship, Drug ; Isoniazid - therapeutic use ; Klebsiella pneumoniae ; Mice ; Microbial Sensitivity Tests ; Mycobacterium tuberculosis ; Rifampin - analogs & derivatives ; Rifampin - metabolism ; Rifampin - pharmacology ; Rifampin - therapeutic use ; Streptococcus pneumoniae ; Streptococcus pyogenes ; Tuberculosis - drug therapy</subject><ispartof>The Journal of Antibiotics, 1981, Vol.34(8), pp.1026-1032</ispartof><rights>Japan Antibiotics Research Association</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c5836-c532de3fd488c657ff899ce631895b44301d477b41c0d0d3e12ac39cd61e878a3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,1882,4024,27923,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7319918$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>ARIOLI, VITTORIO</creatorcontrib><creatorcontrib>BERTI, MARISA</creatorcontrib><creatorcontrib>CARNITI, GIULIANA</creatorcontrib><creatorcontrib>RANDISI, ELEONORA</creatorcontrib><creatorcontrib>ROSSI, ELSA</creatorcontrib><creatorcontrib>SCOTTI, ROBERTO</creatorcontrib><title>ANTIBACTERIAL ACTIVITY OF DL 473, A NEW SEMISYNTHETIC RIFAMYCIN DERIVATIVE</title><title>Journal of antibiotics</title><addtitle>J. Antibiot.</addtitle><description>DL 473, a new semisynthetic rifamycin, was 2-10 times more active in vitro than rifampicin (RAMP) against several clinical isolates of Mycobacterium tuberculosis and only slightly less active than RAMP against Gram-positive and Gram-negative bacteria. It showed excellent therapeutic activity in mice in experimental infections caused by Staphylococcus aureus, Streptococcus pyogenes group A, Streptococcus pneumoniae and Klebsiella pneumoniae. In the experimental TB infection in the mouse DL 473 was clearly more active than isoniazide and RAMP, two of the most effective antitubercular drugs in current use. The LD50 in the mouse was significantly higher than that of RAMP and the half-life was about 5 times longer than that of RAMP.</description><subject>Animals</subject><subject>Anti-Bacterial Agents - pharmacology</subject><subject>Bacteria - drug effects</subject><subject>Bacterial Infections - drug therapy</subject><subject>Dose-Response Relationship, Drug</subject><subject>Isoniazid - therapeutic use</subject><subject>Klebsiella pneumoniae</subject><subject>Mice</subject><subject>Microbial Sensitivity Tests</subject><subject>Mycobacterium tuberculosis</subject><subject>Rifampin - analogs & derivatives</subject><subject>Rifampin - metabolism</subject><subject>Rifampin - pharmacology</subject><subject>Rifampin - therapeutic use</subject><subject>Streptococcus pneumoniae</subject><subject>Streptococcus pyogenes</subject><subject>Tuberculosis - drug therapy</subject><issn>0021-8820</issn><issn>1881-1469</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1981</creationdate><recordtype>article</recordtype><recordid>eNqNkT1v2zAURYmiReKm-QVFAU6dapdPjyKfRlWRGxaKAyRKCk8ETVGpAn-koj3031eGDSNbuzwSuOee5TL2EcREg5Jf3XrbLbrNtvNxgnICIlFv2AiIYAxSZW_ZSIgExkSJOGfvY3wWAjVqOmNnGiHLgEbsRz6rzbe8qMs7k1d8-JhHU8_57ZRfVVxq_MJzPit_8vvyxtzPZ_V1WZuC35lpfjMvzIxfDcXHfGiVH9i71i1juDy-F-xhWtbF9bi6_W6KvBr7lFANF5MmYNtIIq9S3baUZT4oBMrShZQooJFaLyR40YgGAyTOY-YbBYE0Obxgnw_el37zexfi1q666MNy6dZhs4tWI6VSgfgnCCmqVGj6H1CmkmAA8QD6fhNjH1r70ncr1_-xIOx-E_tqE4vS7jcZWp-O-t1iFZpT5zjCkFeH_Dlu3VM45a4fNMvw2gmZor33ePb6E-Z_ud6GNf4FdvGd_w</recordid><startdate>1981</startdate><enddate>1981</enddate><creator>ARIOLI, VITTORIO</creator><creator>BERTI, MARISA</creator><creator>CARNITI, GIULIANA</creator><creator>RANDISI, ELEONORA</creator><creator>ROSSI, ELSA</creator><creator>SCOTTI, ROBERTO</creator><general>JAPAN ANTIBIOTICS RESEARCH ASSOCIATION</general><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>7QL</scope><scope>7T7</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>1981</creationdate><title>ANTIBACTERIAL ACTIVITY OF DL 473, A NEW SEMISYNTHETIC RIFAMYCIN DERIVATIVE</title><author>ARIOLI, VITTORIO ; BERTI, MARISA ; CARNITI, GIULIANA ; RANDISI, ELEONORA ; ROSSI, ELSA ; SCOTTI, ROBERTO</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5836-c532de3fd488c657ff899ce631895b44301d477b41c0d0d3e12ac39cd61e878a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1981</creationdate><topic>Animals</topic><topic>Anti-Bacterial Agents - pharmacology</topic><topic>Bacteria - drug effects</topic><topic>Bacterial Infections - drug therapy</topic><topic>Dose-Response Relationship, Drug</topic><topic>Isoniazid - therapeutic use</topic><topic>Klebsiella pneumoniae</topic><topic>Mice</topic><topic>Microbial Sensitivity Tests</topic><topic>Mycobacterium tuberculosis</topic><topic>Rifampin - analogs & derivatives</topic><topic>Rifampin - metabolism</topic><topic>Rifampin - pharmacology</topic><topic>Rifampin - therapeutic use</topic><topic>Streptococcus pneumoniae</topic><topic>Streptococcus pyogenes</topic><topic>Tuberculosis - drug therapy</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>ARIOLI, VITTORIO</creatorcontrib><creatorcontrib>BERTI, MARISA</creatorcontrib><creatorcontrib>CARNITI, GIULIANA</creatorcontrib><creatorcontrib>RANDISI, ELEONORA</creatorcontrib><creatorcontrib>ROSSI, ELSA</creatorcontrib><creatorcontrib>SCOTTI, ROBERTO</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Bacteriology Abstracts (Microbiology B)</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>ARIOLI, VITTORIO</au><au>BERTI, MARISA</au><au>CARNITI, GIULIANA</au><au>RANDISI, ELEONORA</au><au>ROSSI, ELSA</au><au>SCOTTI, ROBERTO</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>ANTIBACTERIAL ACTIVITY OF DL 473, A NEW SEMISYNTHETIC RIFAMYCIN DERIVATIVE</atitle><jtitle>Journal of antibiotics</jtitle><addtitle>J. Antibiot.</addtitle><date>1981</date><risdate>1981</risdate><volume>34</volume><issue>8</issue><spage>1026</spage><epage>1032</epage><pages>1026-1032</pages><issn>0021-8820</issn><eissn>1881-1469</eissn><abstract>DL 473, a new semisynthetic rifamycin, was 2-10 times more active in vitro than rifampicin (RAMP) against several clinical isolates of Mycobacterium tuberculosis and only slightly less active than RAMP against Gram-positive and Gram-negative bacteria. It showed excellent therapeutic activity in mice in experimental infections caused by Staphylococcus aureus, Streptococcus pyogenes group A, Streptococcus pneumoniae and Klebsiella pneumoniae. In the experimental TB infection in the mouse DL 473 was clearly more active than isoniazide and RAMP, two of the most effective antitubercular drugs in current use. The LD50 in the mouse was significantly higher than that of RAMP and the half-life was about 5 times longer than that of RAMP.</abstract><cop>Japan</cop><pub>JAPAN ANTIBIOTICS RESEARCH ASSOCIATION</pub><pmid>7319918</pmid><doi>10.7164/antibiotics.34.1026</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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ispartof | The Journal of Antibiotics, 1981, Vol.34(8), pp.1026-1032 |
issn | 0021-8820 1881-1469 |
language | eng |
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source | J-STAGE Free - English |
subjects | Animals Anti-Bacterial Agents - pharmacology Bacteria - drug effects Bacterial Infections - drug therapy Dose-Response Relationship, Drug Isoniazid - therapeutic use Klebsiella pneumoniae Mice Microbial Sensitivity Tests Mycobacterium tuberculosis Rifampin - analogs & derivatives Rifampin - metabolism Rifampin - pharmacology Rifampin - therapeutic use Streptococcus pneumoniae Streptococcus pyogenes Tuberculosis - drug therapy |
title | ANTIBACTERIAL ACTIVITY OF DL 473, A NEW SEMISYNTHETIC RIFAMYCIN DERIVATIVE |
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