Synthesis and evaluation for biological activity of 3-alkyl and 3-halogenoalkyl-quinoxalin-2-ones variously substituted. Part 4
A new series of 3-isopropyl-, 3-trifluoromethyl- and 3-bromomethylquinoxaline-2-ones variously substituted on the benzo-moiety were synthesized and submitted to a preliminary in vitro evaluation for antibacterial, antifungal and anti-HIV activities. Furthermore, all compounds were also tested for cy...
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| Veröffentlicht in: | Farmaco (Società chimica italiana : 1989) 2002, Vol.57 (1), p.19-25 |
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| container_title | Farmaco (Società chimica italiana : 1989) |
| container_volume | 57 |
| creator | Carta, Antonio Sanna, Paolo Loriga, Mario Setzu, Maria Giovanna La Colla, Paolo Loddo, Roberta |
| description | A new series of 3-isopropyl-, 3-trifluoromethyl- and 3-bromomethylquinoxaline-2-ones variously substituted on the benzo-moiety were synthesized and submitted to a preliminary in vitro evaluation for antibacterial, antifungal and anti-HIV activities. Furthermore, all compounds were also tested for cytotoxicity. Results of the screening showed that compound
10 exhibits moderate antimicrobial activity against
Staphylococcus aureus (MIC=33 μM), and that
25 and
26 showed interesting cytotoxicity versus mock-infected MT-4 cells. All the other compounds were inactive. |
| doi_str_mv | 10.1016/S0014-827X(01)01153-3 |
| format | Article |
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10 exhibits moderate antimicrobial activity against
Staphylococcus aureus (MIC=33 μM), and that
25 and
26 showed interesting cytotoxicity versus mock-infected MT-4 cells. All the other compounds were inactive.</description><identifier>ISSN: 0014-827X</identifier><identifier>EISSN: 1879-0569</identifier><identifier>DOI: 10.1016/S0014-827X(01)01153-3</identifier><identifier>PMID: 11902641</identifier><language>eng</language><publisher>Lausanne: Elsevier SAS</publisher><subject>2-Quinoxalinones ; Anti-Infective Agents - chemical synthesis ; Anti-Infective Agents - chemistry ; Anti-Infective Agents - pharmacology ; Antibacterial agents ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antifungal Agents - chemical synthesis ; Antifungal Agents - chemistry ; Antifungal Agents - pharmacology ; Antimicrobial activity ; Antiviral agents ; Antiviral Agents - chemical synthesis ; Antiviral Agents - chemistry ; Antiviral Agents - pharmacology ; Biological and medical sciences ; Cell Line - drug effects ; Cytotoxic activity ; Dose-Response Relationship, Drug ; HIV - drug effects ; Humans ; Linear Models ; Medical sciences ; Microbial Sensitivity Tests ; Pharmacology. Drug treatments ; Quinoxalines - chemical synthesis ; Quinoxalines - chemistry ; Quinoxalines - pharmacology ; Structure-Activity Relationship</subject><ispartof>Farmaco (Società chimica italiana : 1989), 2002, Vol.57 (1), p.19-25</ispartof><rights>2002 Elsevier Science S.A.</rights><rights>2002 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c457t-3a2e22bc4571bf3f057bcb616780345c0361fd0607aa79827867c300180983913</citedby><cites>FETCH-LOGICAL-c457t-3a2e22bc4571bf3f057bcb616780345c0361fd0607aa79827867c300180983913</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,4022,27921,27922,27923</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=13627653$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11902641$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Carta, Antonio</creatorcontrib><creatorcontrib>Sanna, Paolo</creatorcontrib><creatorcontrib>Loriga, Mario</creatorcontrib><creatorcontrib>Setzu, Maria Giovanna</creatorcontrib><creatorcontrib>La Colla, Paolo</creatorcontrib><creatorcontrib>Loddo, Roberta</creatorcontrib><title>Synthesis and evaluation for biological activity of 3-alkyl and 3-halogenoalkyl-quinoxalin-2-ones variously substituted. Part 4</title><title>Farmaco (Società chimica italiana : 1989)</title><addtitle>Farmaco</addtitle><description>A new series of 3-isopropyl-, 3-trifluoromethyl- and 3-bromomethylquinoxaline-2-ones variously substituted on the benzo-moiety were synthesized and submitted to a preliminary in vitro evaluation for antibacterial, antifungal and anti-HIV activities. Furthermore, all compounds were also tested for cytotoxicity. Results of the screening showed that compound
10 exhibits moderate antimicrobial activity against
Staphylococcus aureus (MIC=33 μM), and that
25 and
26 showed interesting cytotoxicity versus mock-infected MT-4 cells. All the other compounds were inactive.</description><subject>2-Quinoxalinones</subject><subject>Anti-Infective Agents - chemical synthesis</subject><subject>Anti-Infective Agents - chemistry</subject><subject>Anti-Infective Agents - pharmacology</subject><subject>Antibacterial agents</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antifungal Agents - chemical synthesis</subject><subject>Antifungal Agents - chemistry</subject><subject>Antifungal Agents - pharmacology</subject><subject>Antimicrobial activity</subject><subject>Antiviral agents</subject><subject>Antiviral Agents - chemical synthesis</subject><subject>Antiviral Agents - chemistry</subject><subject>Antiviral Agents - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Cell Line - drug effects</subject><subject>Cytotoxic activity</subject><subject>Dose-Response Relationship, Drug</subject><subject>HIV - drug effects</subject><subject>Humans</subject><subject>Linear Models</subject><subject>Medical sciences</subject><subject>Microbial Sensitivity Tests</subject><subject>Pharmacology. Drug treatments</subject><subject>Quinoxalines - chemical synthesis</subject><subject>Quinoxalines - chemistry</subject><subject>Quinoxalines - pharmacology</subject><subject>Structure-Activity Relationship</subject><issn>0014-827X</issn><issn>1879-0569</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2002</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1rFTEUhoMo9rb6E5RslLpIzZnMJDMrkeIXFBSq4C6cyWRsNDdpk8zFu_Kvm_uBXboKJzzv-XgIeQb8AjjI19ecQ8v6Rn0_5_CKA3SCiQdkBb0aGO_k8JCs_iEn5DTnn7VUSqrH5ARg4I1sYUX-XG9DubHZZYphonaDfsHiYqBzTHR00ccfzqCnaIrbuLKlcaaCof-19fuEYDdYGRvi_o_dLS7E3-hdYA2LwWa6weTikv2W5mXMxZWl2OmCfsFUaPuEPJrRZ_v0-J6Rb-_ffb38yK4-f_h0-faKmbZThQlsbNOMuwLGWcy8U6MZJUjVc9F2hgsJ88QlV4hqqCf3UhlRD-750IsBxBl5eeh7m-LdYnPRa5eN9R6DrctpBV3L-aAq2B1Ak2LOyc76Nrk1pq0Grnfm9d683mnVHPTevBY19_w4YBnXdrpPHVVX4MURwFyFzgmDcfmeE7JRsts1enPgbNWxcTbpbJwNxk4uWVP0FN1_VvkLY3OgZQ</recordid><startdate>2002</startdate><enddate>2002</enddate><creator>Carta, Antonio</creator><creator>Sanna, Paolo</creator><creator>Loriga, Mario</creator><creator>Setzu, Maria Giovanna</creator><creator>La Colla, Paolo</creator><creator>Loddo, Roberta</creator><general>Elsevier SAS</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>2002</creationdate><title>Synthesis and evaluation for biological activity of 3-alkyl and 3-halogenoalkyl-quinoxalin-2-ones variously substituted. Part 4</title><author>Carta, Antonio ; Sanna, Paolo ; Loriga, Mario ; Setzu, Maria Giovanna ; La Colla, Paolo ; Loddo, Roberta</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c457t-3a2e22bc4571bf3f057bcb616780345c0361fd0607aa79827867c300180983913</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2002</creationdate><topic>2-Quinoxalinones</topic><topic>Anti-Infective Agents - chemical synthesis</topic><topic>Anti-Infective Agents - chemistry</topic><topic>Anti-Infective Agents - pharmacology</topic><topic>Antibacterial agents</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antifungal Agents - chemical synthesis</topic><topic>Antifungal Agents - chemistry</topic><topic>Antifungal Agents - pharmacology</topic><topic>Antimicrobial activity</topic><topic>Antiviral agents</topic><topic>Antiviral Agents - chemical synthesis</topic><topic>Antiviral Agents - chemistry</topic><topic>Antiviral Agents - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Cell Line - drug effects</topic><topic>Cytotoxic activity</topic><topic>Dose-Response Relationship, Drug</topic><topic>HIV - drug effects</topic><topic>Humans</topic><topic>Linear Models</topic><topic>Medical sciences</topic><topic>Microbial Sensitivity Tests</topic><topic>Pharmacology. Drug treatments</topic><topic>Quinoxalines - chemical synthesis</topic><topic>Quinoxalines - chemistry</topic><topic>Quinoxalines - pharmacology</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Carta, Antonio</creatorcontrib><creatorcontrib>Sanna, Paolo</creatorcontrib><creatorcontrib>Loriga, Mario</creatorcontrib><creatorcontrib>Setzu, Maria Giovanna</creatorcontrib><creatorcontrib>La Colla, Paolo</creatorcontrib><creatorcontrib>Loddo, Roberta</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>MEDLINE - Academic</collection><jtitle>Farmaco (Società chimica italiana : 1989)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Carta, Antonio</au><au>Sanna, Paolo</au><au>Loriga, Mario</au><au>Setzu, Maria Giovanna</au><au>La Colla, Paolo</au><au>Loddo, Roberta</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and evaluation for biological activity of 3-alkyl and 3-halogenoalkyl-quinoxalin-2-ones variously substituted. 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10 exhibits moderate antimicrobial activity against
Staphylococcus aureus (MIC=33 μM), and that
25 and
26 showed interesting cytotoxicity versus mock-infected MT-4 cells. All the other compounds were inactive.</abstract><cop>Lausanne</cop><pub>Elsevier SAS</pub><pmid>11902641</pmid><doi>10.1016/S0014-827X(01)01153-3</doi><tpages>7</tpages></addata></record> |
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| ispartof | Farmaco (Società chimica italiana : 1989), 2002, Vol.57 (1), p.19-25 |
| issn | 0014-827X 1879-0569 |
| language | eng |
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| source | MEDLINE; Alma/SFX Local Collection |
| subjects | 2-Quinoxalinones Anti-Infective Agents - chemical synthesis Anti-Infective Agents - chemistry Anti-Infective Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal Agents - chemical synthesis Antifungal Agents - chemistry Antifungal Agents - pharmacology Antimicrobial activity Antiviral agents Antiviral Agents - chemical synthesis Antiviral Agents - chemistry Antiviral Agents - pharmacology Biological and medical sciences Cell Line - drug effects Cytotoxic activity Dose-Response Relationship, Drug HIV - drug effects Humans Linear Models Medical sciences Microbial Sensitivity Tests Pharmacology. Drug treatments Quinoxalines - chemical synthesis Quinoxalines - chemistry Quinoxalines - pharmacology Structure-Activity Relationship |
| title | Synthesis and evaluation for biological activity of 3-alkyl and 3-halogenoalkyl-quinoxalin-2-ones variously substituted. Part 4 |
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