Effect of ruthenium complexation on trypanocidal activity of 5-nitrofuryl containing thiosemicarbazones
In the search of new therapeutic tools for the treatment of American Trypanosomiasis, the largest parasitic disease burden in the American continent, three series of novel ruthenium complexes of the formula [RuCl 2(HL) 2], [RuCl 3(dmso)(HL)] and [RuCl(PPh 3)(L) 2] with bioactive 5-nitrofuryl contain...
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| Veröffentlicht in: | European journal of medicinal chemistry 2009-12, Vol.44 (12), p.4937-4943 |
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| container_title | European journal of medicinal chemistry |
| container_volume | 44 |
| creator | Pagano, Mariana Demoro, Bruno Toloza, Jeanette Boiani, Lucía González, Mercedes Cerecetto, Hugo Olea-Azar, Claudio Norambuena, Ester Gambino, Dinorah Otero, Lucía |
| description | In the search of new therapeutic tools for the treatment of American Trypanosomiasis, the largest parasitic disease burden in the American continent, three series of novel ruthenium complexes of the formula [RuCl
2(HL)
2], [RuCl
3(dmso)(HL)] and [RuCl(PPh
3)(L)
2] with bioactive 5-nitrofuryl containing thiosemicarbazones as ligands (HL neutral, L monoanionic) were synthesized and characterized. Their
in vitro growth inhibition activity against
Trypanosoma cruzi and the effect of co-ligands in related physicochemical properties
i.e. nitro moiety redox potential, lipophilicity and free radical scavenger capacity were evaluated. Results show that although a loss of activity was observed as a consequence of ruthenium complexation, lipophilicity and free radical scavenger capacity of the obtained complexes could be correlated to their trypanocidal effect.
[Display omitted] Ruthenium complexes of the formula [Ru
IICl
2(HL)
2], [Ru
IIICl
3(dmso)(HL)] and [Ru
IIICl(PPh
3)(L)
2] with bioactive ligands against Chagas disease were obtained. The effect of co-ligands on the biological activity and related physicochemical properties resulted evident. |
| doi_str_mv | 10.1016/j.ejmech.2009.08.008 |
| format | Article |
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2(HL)
2], [RuCl
3(dmso)(HL)] and [RuCl(PPh
3)(L)
2] with bioactive 5-nitrofuryl containing thiosemicarbazones as ligands (HL neutral, L monoanionic) were synthesized and characterized. Their
in vitro growth inhibition activity against
Trypanosoma cruzi and the effect of co-ligands in related physicochemical properties
i.e. nitro moiety redox potential, lipophilicity and free radical scavenger capacity were evaluated. Results show that although a loss of activity was observed as a consequence of ruthenium complexation, lipophilicity and free radical scavenger capacity of the obtained complexes could be correlated to their trypanocidal effect.
[Display omitted] Ruthenium complexes of the formula [Ru
IICl
2(HL)
2], [Ru
IIICl
3(dmso)(HL)] and [Ru
IIICl(PPh
3)(L)
2] with bioactive ligands against Chagas disease were obtained. The effect of co-ligands on the biological activity and related physicochemical properties resulted evident.</description><identifier>ISSN: 0223-5234</identifier><identifier>EISSN: 1768-3254</identifier><identifier>DOI: 10.1016/j.ejmech.2009.08.008</identifier><identifier>PMID: 19783078</identifier><identifier>CODEN: EJMCA5</identifier><language>eng</language><publisher>Kidlington: Elsevier Masson SAS</publisher><subject>5-Nitrofuryl containing thiosemicarbazones ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antiparasitic agents ; Biological and medical sciences ; Chagas disease ; Ligands ; Medical sciences ; Molecular Structure ; Nitrofurans - chemistry ; Nitrofurans - pharmacology ; Organometallic Compounds - chemical synthesis ; Organometallic Compounds - chemistry ; Organometallic Compounds - pharmacology ; Pharmacology. Drug treatments ; Ruthenium - chemistry ; Ruthenium - pharmacology ; Ruthenium complexes ; Thiosemicarbazones - chemistry ; Thiosemicarbazones - pharmacology ; Trypanocidal Agents - chemical synthesis ; Trypanocidal Agents - chemistry ; Trypanocidal Agents - pharmacology ; Trypanosoma cruzi - drug effects</subject><ispartof>European journal of medicinal chemistry, 2009-12, Vol.44 (12), p.4937-4943</ispartof><rights>2009 Elsevier Masson SAS</rights><rights>2015 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c391t-b8b35f3b3d75fb9fcd65b9682c0ec14e7d61f8c1137049b4e5deda60184d6883</citedby><cites>FETCH-LOGICAL-c391t-b8b35f3b3d75fb9fcd65b9682c0ec14e7d61f8c1137049b4e5deda60184d6883</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.ejmech.2009.08.008$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=22280559$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19783078$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Pagano, Mariana</creatorcontrib><creatorcontrib>Demoro, Bruno</creatorcontrib><creatorcontrib>Toloza, Jeanette</creatorcontrib><creatorcontrib>Boiani, Lucía</creatorcontrib><creatorcontrib>González, Mercedes</creatorcontrib><creatorcontrib>Cerecetto, Hugo</creatorcontrib><creatorcontrib>Olea-Azar, Claudio</creatorcontrib><creatorcontrib>Norambuena, Ester</creatorcontrib><creatorcontrib>Gambino, Dinorah</creatorcontrib><creatorcontrib>Otero, Lucía</creatorcontrib><title>Effect of ruthenium complexation on trypanocidal activity of 5-nitrofuryl containing thiosemicarbazones</title><title>European journal of medicinal chemistry</title><addtitle>Eur J Med Chem</addtitle><description>In the search of new therapeutic tools for the treatment of American Trypanosomiasis, the largest parasitic disease burden in the American continent, three series of novel ruthenium complexes of the formula [RuCl
2(HL)
2], [RuCl
3(dmso)(HL)] and [RuCl(PPh
3)(L)
2] with bioactive 5-nitrofuryl containing thiosemicarbazones as ligands (HL neutral, L monoanionic) were synthesized and characterized. Their
in vitro growth inhibition activity against
Trypanosoma cruzi and the effect of co-ligands in related physicochemical properties
i.e. nitro moiety redox potential, lipophilicity and free radical scavenger capacity were evaluated. Results show that although a loss of activity was observed as a consequence of ruthenium complexation, lipophilicity and free radical scavenger capacity of the obtained complexes could be correlated to their trypanocidal effect.
[Display omitted] Ruthenium complexes of the formula [Ru
IICl
2(HL)
2], [Ru
IIICl
3(dmso)(HL)] and [Ru
IIICl(PPh
3)(L)
2] with bioactive ligands against Chagas disease were obtained. The effect of co-ligands on the biological activity and related physicochemical properties resulted evident.</description><subject>5-Nitrofuryl containing thiosemicarbazones</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antiparasitic agents</subject><subject>Biological and medical sciences</subject><subject>Chagas disease</subject><subject>Ligands</subject><subject>Medical sciences</subject><subject>Molecular Structure</subject><subject>Nitrofurans - chemistry</subject><subject>Nitrofurans - pharmacology</subject><subject>Organometallic Compounds - chemical synthesis</subject><subject>Organometallic Compounds - chemistry</subject><subject>Organometallic Compounds - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Ruthenium - chemistry</subject><subject>Ruthenium - pharmacology</subject><subject>Ruthenium complexes</subject><subject>Thiosemicarbazones - chemistry</subject><subject>Thiosemicarbazones - pharmacology</subject><subject>Trypanocidal Agents - chemical synthesis</subject><subject>Trypanocidal Agents - chemistry</subject><subject>Trypanocidal Agents - pharmacology</subject><subject>Trypanosoma cruzi - drug effects</subject><issn>0223-5234</issn><issn>1768-3254</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kcFq3DAQhkVoSTZp36AUX0pOdkeSZcuXQglJUwj0kruQpVFWiy1tJTl0-_T1skt7KwzM5ftnhm8I-UChoUC7z7sGdzOabcMAhgZkAyAvyIb2naw5E-0bsgHGeC0Yb6_Idc47ABAdwCW5okMvOfRyQ17unUNTquiqtJQtBr_MlYnzfsJfuvgYqrVKOux1iMZbPVXaFP_qy-EYEXXwJUW3pMO0pkLRPvjwUpWtjxlnb3Qa9e8YML8jb52eMr4_9xvy_HD_fPdYP_349v3u61Nt-EBLPcqRC8dHbnvhxsEZ24lx6CQzgIa22NuOOmko5T20w9iisGh1B1S2tpOS35Db09h9ij8XzEXNPhucJh0wLln1nPcUBnYk2xNpUsw5oVP75GedDoqCOgpWO3USrI6CFUi1Cl5jH88LlnFG-y90NroCn86AzkZPLulgfP7LMcYkCDGs3JcTh6uNV49JZeMxGLQ-rQ9RNvr_X_IHfwudtQ</recordid><startdate>20091201</startdate><enddate>20091201</enddate><creator>Pagano, Mariana</creator><creator>Demoro, Bruno</creator><creator>Toloza, Jeanette</creator><creator>Boiani, Lucía</creator><creator>González, Mercedes</creator><creator>Cerecetto, Hugo</creator><creator>Olea-Azar, Claudio</creator><creator>Norambuena, Ester</creator><creator>Gambino, Dinorah</creator><creator>Otero, Lucía</creator><general>Elsevier Masson SAS</general><general>Elsevier</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>20091201</creationdate><title>Effect of ruthenium complexation on trypanocidal activity of 5-nitrofuryl containing thiosemicarbazones</title><author>Pagano, Mariana ; Demoro, Bruno ; Toloza, Jeanette ; Boiani, Lucía ; González, Mercedes ; Cerecetto, Hugo ; Olea-Azar, Claudio ; Norambuena, Ester ; Gambino, Dinorah ; Otero, Lucía</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c391t-b8b35f3b3d75fb9fcd65b9682c0ec14e7d61f8c1137049b4e5deda60184d6883</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>5-Nitrofuryl containing thiosemicarbazones</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antiparasitic agents</topic><topic>Biological and medical sciences</topic><topic>Chagas disease</topic><topic>Ligands</topic><topic>Medical sciences</topic><topic>Molecular Structure</topic><topic>Nitrofurans - chemistry</topic><topic>Nitrofurans - pharmacology</topic><topic>Organometallic Compounds - chemical synthesis</topic><topic>Organometallic Compounds - chemistry</topic><topic>Organometallic Compounds - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Ruthenium - chemistry</topic><topic>Ruthenium - pharmacology</topic><topic>Ruthenium complexes</topic><topic>Thiosemicarbazones - chemistry</topic><topic>Thiosemicarbazones - pharmacology</topic><topic>Trypanocidal Agents - chemical synthesis</topic><topic>Trypanocidal Agents - chemistry</topic><topic>Trypanocidal Agents - pharmacology</topic><topic>Trypanosoma cruzi - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Pagano, Mariana</creatorcontrib><creatorcontrib>Demoro, Bruno</creatorcontrib><creatorcontrib>Toloza, Jeanette</creatorcontrib><creatorcontrib>Boiani, Lucía</creatorcontrib><creatorcontrib>González, Mercedes</creatorcontrib><creatorcontrib>Cerecetto, Hugo</creatorcontrib><creatorcontrib>Olea-Azar, Claudio</creatorcontrib><creatorcontrib>Norambuena, Ester</creatorcontrib><creatorcontrib>Gambino, Dinorah</creatorcontrib><creatorcontrib>Otero, Lucía</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>European journal of medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Pagano, Mariana</au><au>Demoro, Bruno</au><au>Toloza, Jeanette</au><au>Boiani, Lucía</au><au>González, Mercedes</au><au>Cerecetto, Hugo</au><au>Olea-Azar, Claudio</au><au>Norambuena, Ester</au><au>Gambino, Dinorah</au><au>Otero, Lucía</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of ruthenium complexation on trypanocidal activity of 5-nitrofuryl containing thiosemicarbazones</atitle><jtitle>European journal of medicinal chemistry</jtitle><addtitle>Eur J Med Chem</addtitle><date>2009-12-01</date><risdate>2009</risdate><volume>44</volume><issue>12</issue><spage>4937</spage><epage>4943</epage><pages>4937-4943</pages><issn>0223-5234</issn><eissn>1768-3254</eissn><coden>EJMCA5</coden><abstract>In the search of new therapeutic tools for the treatment of American Trypanosomiasis, the largest parasitic disease burden in the American continent, three series of novel ruthenium complexes of the formula [RuCl
2(HL)
2], [RuCl
3(dmso)(HL)] and [RuCl(PPh
3)(L)
2] with bioactive 5-nitrofuryl containing thiosemicarbazones as ligands (HL neutral, L monoanionic) were synthesized and characterized. Their
in vitro growth inhibition activity against
Trypanosoma cruzi and the effect of co-ligands in related physicochemical properties
i.e. nitro moiety redox potential, lipophilicity and free radical scavenger capacity were evaluated. Results show that although a loss of activity was observed as a consequence of ruthenium complexation, lipophilicity and free radical scavenger capacity of the obtained complexes could be correlated to their trypanocidal effect.
[Display omitted] Ruthenium complexes of the formula [Ru
IICl
2(HL)
2], [Ru
IIICl
3(dmso)(HL)] and [Ru
IIICl(PPh
3)(L)
2] with bioactive ligands against Chagas disease were obtained. The effect of co-ligands on the biological activity and related physicochemical properties resulted evident.</abstract><cop>Kidlington</cop><pub>Elsevier Masson SAS</pub><pmid>19783078</pmid><doi>10.1016/j.ejmech.2009.08.008</doi><tpages>7</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0223-5234 |
| ispartof | European journal of medicinal chemistry, 2009-12, Vol.44 (12), p.4937-4943 |
| issn | 0223-5234 1768-3254 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | 5-Nitrofuryl containing thiosemicarbazones Antibiotics. Antiinfectious agents. Antiparasitic agents Antiparasitic agents Biological and medical sciences Chagas disease Ligands Medical sciences Molecular Structure Nitrofurans - chemistry Nitrofurans - pharmacology Organometallic Compounds - chemical synthesis Organometallic Compounds - chemistry Organometallic Compounds - pharmacology Pharmacology. Drug treatments Ruthenium - chemistry Ruthenium - pharmacology Ruthenium complexes Thiosemicarbazones - chemistry Thiosemicarbazones - pharmacology Trypanocidal Agents - chemical synthesis Trypanocidal Agents - chemistry Trypanocidal Agents - pharmacology Trypanosoma cruzi - drug effects |
| title | Effect of ruthenium complexation on trypanocidal activity of 5-nitrofuryl containing thiosemicarbazones |
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