Synthesis and structure–activity relationship of 7-(substituted)-aminomethyl-4-quinolone-3-carboxylic acid derivatives
Gram-positive organisms have re-emerged as the major hospital pathogens, which make the unmet medical needs for antibacterial therapy even worse. In searching for potent agents against Gram-positive pathogens, novel 7-(substituted)-aminomethyl-quinolone-3-carboxylic acids were designed, synthesized,...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2007-12, Vol.15 (23), p.7274-7280 |
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| container_title | Bioorganic & medicinal chemistry |
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| creator | Zhang, Zhenfa Yu, Aizhen Zhou, Weicheng |
| description | Gram-positive organisms have re-emerged as the major hospital pathogens, which make the unmet medical needs for antibacterial therapy even worse. In searching for potent agents against Gram-positive pathogens, novel 7-(substituted)-aminomethyl-quinolone-3-carboxylic acids were designed, synthesized, and evaluated for their antibacterial activities in vitro. Many 7-monoarylaminomethyl derivatives exhibited high potency against Gram-positive organisms compared to reference agents: vancomycin and pazufloxacin. Additionally, a few 7-monoalkylaminomethyl derivatives exhibited good activities against both Gram-positive and Gram-negative organisms. |
| doi_str_mv | 10.1016/j.bmc.2007.08.031 |
| format | Article |
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In searching for potent agents against Gram-positive pathogens, novel 7-(substituted)-aminomethyl-quinolone-3-carboxylic acids were designed, synthesized, and evaluated for their antibacterial activities in vitro. Many 7-monoarylaminomethyl derivatives exhibited high potency against Gram-positive organisms compared to reference agents: vancomycin and pazufloxacin. Additionally, a few 7-monoalkylaminomethyl derivatives exhibited good activities against both Gram-positive and Gram-negative organisms.</description><subject>Anti-Bacterial Agents - chemical synthesis</subject><subject>Anti-Bacterial Agents - chemistry</subject><subject>Anti-Bacterial Agents - pharmacology</subject><subject>Antibacterial agent</subject><subject>Antibacterial agents</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Biological and medical sciences</subject><subject>Carboxylic Acids - chemical synthesis</subject><subject>Carboxylic Acids - chemistry</subject><subject>Carboxylic Acids - pharmacology</subject><subject>Drug Design</subject><subject>Fluoroquinolones</subject><subject>Gram-positive bacteria</subject><subject>Klebsiella pneumoniae - drug effects</subject><subject>Medical sciences</subject><subject>Microbial Sensitivity Tests</subject><subject>Molecular Structure</subject><subject>Pharmacology. Drug treatments</subject><subject>Quinolones - chemical synthesis</subject><subject>Quinolones - chemistry</subject><subject>Quinolones - pharmacology</subject><subject>Salmonella - drug effects</subject><subject>Shigella boydii - drug effects</subject><subject>Staphylococcus aureus - drug effects</subject><subject>Stereoisomerism</subject><subject>Streptococcus - drug effects</subject><subject>Structure-Activity Relationship</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kM-KFDEQh4Mo7uzqA3iRvih6SFtJptMJnmRxVVjwoJ5DOqlmMvSf2SQ9bN98B9_QJzHLDOzNU1HU9_tRfIS8YlAzYPLDvu5GV3OAtgZVg2BPyIZt5ZYKodlTsgEtFQWl5QW5TGkPAHyr2XNywVrFJeh2Q-5_rFPeYQqpspOvUo6Ly0vEv7__WJfDMeS1ijjYHOYp7cKhmvuqpe_S0qUc8pLRv6d2DNM8Yt6tA93Su6VswzwhFdTZ2M336xBcZV3wlccYjqXriOkFedbbIeHL87wiv24-_7z-Sm-_f_l2_emWOqFYpgy4bCWX3upGgpfOC1SglOo5V5Ip1moG0JQ7NkI3quOud67ljWbSsqYTV-TtqfcQ57sFUzZjSA6HwU44L8lIJZTSvC0gO4EuzilF7M0hhtHG1TAwD7rN3hTd5kG3AWWK7pJ5fS5fuhH9Y-LstwBvzoBNzg59tJML6ZErX7YCmsJ9PHFYVBwDRpNcwMmhDxFdNn4O_3njH7N4n2A</recordid><startdate>20071201</startdate><enddate>20071201</enddate><creator>Zhang, Zhenfa</creator><creator>Yu, Aizhen</creator><creator>Zhou, Weicheng</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><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20071201</creationdate><title>Synthesis and structure–activity relationship of 7-(substituted)-aminomethyl-4-quinolone-3-carboxylic acid derivatives</title><author>Zhang, Zhenfa ; Yu, Aizhen ; Zhou, Weicheng</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c381t-10267626da9560d6cd3e80888f22861817910056dae53958b2cfcc725916a15b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>Anti-Bacterial Agents - chemical synthesis</topic><topic>Anti-Bacterial Agents - chemistry</topic><topic>Anti-Bacterial Agents - pharmacology</topic><topic>Antibacterial agent</topic><topic>Antibacterial agents</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Biological and medical sciences</topic><topic>Carboxylic Acids - chemical synthesis</topic><topic>Carboxylic Acids - chemistry</topic><topic>Carboxylic Acids - pharmacology</topic><topic>Drug Design</topic><topic>Fluoroquinolones</topic><topic>Gram-positive bacteria</topic><topic>Klebsiella pneumoniae - drug effects</topic><topic>Medical sciences</topic><topic>Microbial Sensitivity Tests</topic><topic>Molecular Structure</topic><topic>Pharmacology. 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In searching for potent agents against Gram-positive pathogens, novel 7-(substituted)-aminomethyl-quinolone-3-carboxylic acids were designed, synthesized, and evaluated for their antibacterial activities in vitro. Many 7-monoarylaminomethyl derivatives exhibited high potency against Gram-positive organisms compared to reference agents: vancomycin and pazufloxacin. Additionally, a few 7-monoalkylaminomethyl derivatives exhibited good activities against both Gram-positive and Gram-negative organisms.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>17826097</pmid><doi>10.1016/j.bmc.2007.08.031</doi><tpages>7</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0968-0896 |
| ispartof | Bioorganic & medicinal chemistry, 2007-12, Vol.15 (23), p.7274-7280 |
| issn | 0968-0896 1464-3391 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Antibacterial agent Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Carboxylic Acids - chemical synthesis Carboxylic Acids - chemistry Carboxylic Acids - pharmacology Drug Design Fluoroquinolones Gram-positive bacteria Klebsiella pneumoniae - drug effects Medical sciences Microbial Sensitivity Tests Molecular Structure Pharmacology. Drug treatments Quinolones - chemical synthesis Quinolones - chemistry Quinolones - pharmacology Salmonella - drug effects Shigella boydii - drug effects Staphylococcus aureus - drug effects Stereoisomerism Streptococcus - drug effects Structure-Activity Relationship |
| title | Synthesis and structure–activity relationship of 7-(substituted)-aminomethyl-4-quinolone-3-carboxylic acid derivatives |
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