Novel bisquinoline antimalarials: Synthesis, antimalarial activity, and inhibition of haem polymerisation
We report the synthesis of two series of novel bisquinoline compounds that inhibit the growth of both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. To study the molecular basis of the action of these novel antimalarial drugs, we examined their ability to inhibit h...
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| Veröffentlicht in: | Biochemical pharmacology 1996-08, Vol.52 (4), p.551-559 |
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| container_end_page | 559 |
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| container_title | Biochemical pharmacology |
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| creator | Raynes, Kaylene Foley, Michael Tilley, Leann Deady, Leslie W. |
| description | We report the synthesis of two series of novel bisquinoline compounds that inhibit the growth of both chloroquine-sensitive and chloroquine-resistant strains of
Plasmodium falciparum. To study the molecular basis of the action of these novel antimalarial drugs, we examined their ability to inhibit haem polymerisation in the presence and absence of parasite extracts. The level of antimalarial potency was correlated with the level of inhibition of haem polymerisation, suggesting that these bisquinolines exert their antimalarial activity by antagonising the sequestration of toxic haem moieties. |
| doi_str_mv | 10.1016/0006-2952(96)00306-1 |
| format | Article |
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Plasmodium falciparum. To study the molecular basis of the action of these novel antimalarial drugs, we examined their ability to inhibit haem polymerisation in the presence and absence of parasite extracts. The level of antimalarial potency was correlated with the level of inhibition of haem polymerisation, suggesting that these bisquinolines exert their antimalarial activity by antagonising the sequestration of toxic haem moieties.</description><identifier>ISSN: 0006-2952</identifier><identifier>EISSN: 1873-2968</identifier><identifier>DOI: 10.1016/0006-2952(96)00306-1</identifier><identifier>PMID: 8759027</identifier><identifier>CODEN: BCPCA6</identifier><language>eng</language><publisher>New York, NY: Elsevier Inc</publisher><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antimalarials - chemistry ; Antimalarials - pharmacology ; Antiparasitic agents ; Biological and medical sciences ; bisquinolines ; Chloroquine - chemistry ; Chloroquine - pharmacology ; Dose-Response Relationship, Drug ; drug resistance ; haem polymerisation ; haemozoin ; malaria ; Medical sciences ; Pharmacology. Drug treatments ; Plasmodium falciparum ; quinoline antimalarials ; Quinolines - chemistry ; Quinolines - pharmacology</subject><ispartof>Biochemical pharmacology, 1996-08, Vol.52 (4), p.551-559</ispartof><rights>1996</rights><rights>1996 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0006-2952(96)00306-1$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,778,782,3539,27907,27908,45978</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3186872$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8759027$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Raynes, Kaylene</creatorcontrib><creatorcontrib>Foley, Michael</creatorcontrib><creatorcontrib>Tilley, Leann</creatorcontrib><creatorcontrib>Deady, Leslie W.</creatorcontrib><title>Novel bisquinoline antimalarials: Synthesis, antimalarial activity, and inhibition of haem polymerisation</title><title>Biochemical pharmacology</title><addtitle>Biochem Pharmacol</addtitle><description>We report the synthesis of two series of novel bisquinoline compounds that inhibit the growth of both chloroquine-sensitive and chloroquine-resistant strains of
Plasmodium falciparum. To study the molecular basis of the action of these novel antimalarial drugs, we examined their ability to inhibit haem polymerisation in the presence and absence of parasite extracts. The level of antimalarial potency was correlated with the level of inhibition of haem polymerisation, suggesting that these bisquinolines exert their antimalarial activity by antagonising the sequestration of toxic haem moieties.</description><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antimalarials - chemistry</subject><subject>Antimalarials - pharmacology</subject><subject>Antiparasitic agents</subject><subject>Biological and medical sciences</subject><subject>bisquinolines</subject><subject>Chloroquine - chemistry</subject><subject>Chloroquine - pharmacology</subject><subject>Dose-Response Relationship, Drug</subject><subject>drug resistance</subject><subject>haem polymerisation</subject><subject>haemozoin</subject><subject>malaria</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Plasmodium falciparum</subject><subject>quinoline antimalarials</subject><subject>Quinolines - chemistry</subject><subject>Quinolines - pharmacology</subject><issn>0006-2952</issn><issn>1873-2968</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1996</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpVkVtLxDAQhYMoul7-gUIfRBRczaVNUh8EWbyB6IP6HKbNlB1p07XpLuy_t8VF8Cmccz4mzBzGjgW_Elzoa865nso8k-e5vuBcDUpssYmwRg22ttts8ofssf0Yv0Zptdhlu9ZkOZdmwui1XWGdFBS_lxTamgImEHpqoIaOoI43yfs69HOMFC__JQmUPa2oX4-2TyjMqaCe2pC0VTIHbJJFW68b7CjCaB-ynWqYh0eb94B9Ptx_zJ6mL2-Pz7O7lykqKfopesNz1KkvdIrWWsWt0aA58CxTWlRcqgJQ-0obL4tSZmA8GKlAitSaVKoDdvY7d9G130uMvWsolljXELBdRicyK9Jc8gE82YDLokHvFt2wW7d2m9sM-ekmh1hCXXUQSop_mBJWWzP-d_uL4bDUirBzsSQMJXrqsOydb8kJ7sbK3FiAG_tw-SiGypxQP4Q_iHo</recordid><startdate>19960823</startdate><enddate>19960823</enddate><creator>Raynes, Kaylene</creator><creator>Foley, Michael</creator><creator>Tilley, Leann</creator><creator>Deady, Leslie W.</creator><general>Elsevier Inc</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>M7N</scope></search><sort><creationdate>19960823</creationdate><title>Novel bisquinoline antimalarials: Synthesis, antimalarial activity, and inhibition of haem polymerisation</title><author>Raynes, Kaylene ; Foley, Michael ; Tilley, Leann ; Deady, Leslie W.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-e321t-ed709e64db64e88830876a60a055361f023bae6df67d2bc25a7da723a21487423</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1996</creationdate><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antimalarials - chemistry</topic><topic>Antimalarials - pharmacology</topic><topic>Antiparasitic agents</topic><topic>Biological and medical sciences</topic><topic>bisquinolines</topic><topic>Chloroquine - chemistry</topic><topic>Chloroquine - pharmacology</topic><topic>Dose-Response Relationship, Drug</topic><topic>drug resistance</topic><topic>haem polymerisation</topic><topic>haemozoin</topic><topic>malaria</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Plasmodium falciparum</topic><topic>quinoline antimalarials</topic><topic>Quinolines - chemistry</topic><topic>Quinolines - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Raynes, Kaylene</creatorcontrib><creatorcontrib>Foley, Michael</creatorcontrib><creatorcontrib>Tilley, Leann</creatorcontrib><creatorcontrib>Deady, Leslie W.</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>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><jtitle>Biochemical pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Raynes, Kaylene</au><au>Foley, Michael</au><au>Tilley, Leann</au><au>Deady, Leslie W.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel bisquinoline antimalarials: Synthesis, antimalarial activity, and inhibition of haem polymerisation</atitle><jtitle>Biochemical pharmacology</jtitle><addtitle>Biochem Pharmacol</addtitle><date>1996-08-23</date><risdate>1996</risdate><volume>52</volume><issue>4</issue><spage>551</spage><epage>559</epage><pages>551-559</pages><issn>0006-2952</issn><eissn>1873-2968</eissn><coden>BCPCA6</coden><abstract>We report the synthesis of two series of novel bisquinoline compounds that inhibit the growth of both chloroquine-sensitive and chloroquine-resistant strains of
Plasmodium falciparum. To study the molecular basis of the action of these novel antimalarial drugs, we examined their ability to inhibit haem polymerisation in the presence and absence of parasite extracts. The level of antimalarial potency was correlated with the level of inhibition of haem polymerisation, suggesting that these bisquinolines exert their antimalarial activity by antagonising the sequestration of toxic haem moieties.</abstract><cop>New York, NY</cop><pub>Elsevier Inc</pub><pmid>8759027</pmid><doi>10.1016/0006-2952(96)00306-1</doi><tpages>9</tpages></addata></record> |
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| ispartof | Biochemical pharmacology, 1996-08, Vol.52 (4), p.551-559 |
| issn | 0006-2952 1873-2968 |
| language | eng |
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| source | Elsevier ScienceDirect Journals Complete - AutoHoldings; MEDLINE |
| subjects | Antibiotics. Antiinfectious agents. Antiparasitic agents Antimalarials - chemistry Antimalarials - pharmacology Antiparasitic agents Biological and medical sciences bisquinolines Chloroquine - chemistry Chloroquine - pharmacology Dose-Response Relationship, Drug drug resistance haem polymerisation haemozoin malaria Medical sciences Pharmacology. Drug treatments Plasmodium falciparum quinoline antimalarials Quinolines - chemistry Quinolines - pharmacology |
| title | Novel bisquinoline antimalarials: Synthesis, antimalarial activity, and inhibition of haem polymerisation |
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