Novel N-(4-Piperidinyl)benzamide Antimalarials with Mammalian Protein Farnesyltransferase Inhibitory Activity
Protein farnesyltransferase of Plasmodium falciparum is a potential target in the treatment of malaria for which increased drug resistance is observed. The design, synthesis and evaluation of a series of N-(4-piperidinyl)benzamides is reported. The most potent compounds showed in vitro activity agai...
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| Veröffentlicht in: | Chemical & pharmaceutical bulletin 2005, Vol.53(10), pp.1324-1326 |
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| container_title | Chemical & pharmaceutical bulletin |
| container_volume | 53 |
| creator | Ryckebusch, Adina Gilleron, Pauline Millet, Régis Houssin, Raymond Lemoine, Amélie Pommery, Nicole Grellier, Philippe Sergheraert, Christian Hénichart, Jean-Pierre |
| description | Protein farnesyltransferase of Plasmodium falciparum is a potential target in the treatment of malaria for which increased drug resistance is observed. The design, synthesis and evaluation of a series of N-(4-piperidinyl)benzamides is reported. The most potent compounds showed in vitro activity against the parasite at submicromolar concentrations. |
| doi_str_mv | 10.1248/cpb.53.1324 |
| format | Article |
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The design, synthesis and evaluation of a series of N-(4-piperidinyl)benzamides is reported. 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Pharm. Bull.</addtitle><description>Protein farnesyltransferase of Plasmodium falciparum is a potential target in the treatment of malaria for which increased drug resistance is observed. The design, synthesis and evaluation of a series of N-(4-piperidinyl)benzamides is reported. The most potent compounds showed in vitro activity against the parasite at submicromolar concentrations.</description><subject>Alkyl and Aryl Transferases - antagonists & inhibitors</subject><subject>Animals</subject><subject>Antimalarials - chemical synthesis</subject><subject>Antimalarials - chemistry</subject><subject>Antimalarials - pharmacology</subject><subject>Benzamides - chemical synthesis</subject><subject>Benzamides - chemistry</subject><subject>Benzamides - pharmacology</subject><subject>Cell Line, Tumor</subject><subject>Cell Proliferation - drug effects</subject><subject>Chemical Sciences</subject><subject>Drug Design</subject><subject>Drug Evaluation, Preclinical</subject><subject>Drug Screening Assays, Antitumor</subject><subject>farnesyltransferase</subject><subject>Humans</subject><subject>inhibitor</subject><subject>Life Sciences</subject><subject>malaria</subject><subject>Mice</subject><subject>Microbiology and Parasitology</subject><subject>Molecular Structure</subject><subject>N-(4-piperidinyl)benzamide derivative</subject><subject>Parasitic Sensitivity Tests</subject><subject>Plasmodium falciparum</subject><subject>Plasmodium falciparum - drug effects</subject><subject>Plasmodium falciparum - enzymology</subject><subject>Structure-Activity Relationship</subject><issn>0009-2363</issn><issn>1347-5223</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpd0c2L1DAYBvAgijuunrxLQRA_6Jjvtsdxcd2Fcd2DnsObNLUZ2nQ2yYzUv94MM8yClwSSHw_vy4PQa4KXhPL6s9nqpWBLwih_ghaE8aoUlLKnaIExbkrKJLtAL2LcYEwFrthzdEEkxbxp2AKNd9PeDsVd-Z6X925rg2udn4cP2vq_MLrWFiuf3AgDBAdDLP641BffYcwvDnxxH6ZknS-uIXgb5yEF8LGzAaItbn3vtEtTmIuVSW7v0vwSPetyin11ui_Rr-uvP69uyvWPb7dXq3VpBJOpbHHDOy3BCGxF10KDOYdK67oiVICoK6E7AoLQinLNtBE1tEw01gjBiDCMXaKPx9weBrUNef4wqwmculmt1eh7rzDFFSaE7knG7454G6aHnY1JjS4aOwzg7bSLStZSME5lhm__g5tpF3xeRBEuMasla3hWn47KhCnGYLvzAASrQ2EqF6YEU4fCsn5zytzp0baP9tRQBl-OYBMT_LZnACE5M9hzGD6dh9THzx6Csp79AwfLqFU</recordid><startdate>20051001</startdate><enddate>20051001</enddate><creator>Ryckebusch, Adina</creator><creator>Gilleron, Pauline</creator><creator>Millet, Régis</creator><creator>Houssin, Raymond</creator><creator>Lemoine, Amélie</creator><creator>Pommery, Nicole</creator><creator>Grellier, Philippe</creator><creator>Sergheraert, Christian</creator><creator>Hénichart, Jean-Pierre</creator><general>The Pharmaceutical Society of Japan</general><general>Japan Science and Technology Agency</general><general>Pharmaceutical Society of Japan</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>7TK</scope><scope>7TM</scope><scope>7U9</scope><scope>H94</scope><scope>7X8</scope><scope>1XC</scope><scope>VOOES</scope><orcidid>https://orcid.org/0000-0003-4153-0465</orcidid></search><sort><creationdate>20051001</creationdate><title>Novel N-(4-Piperidinyl)benzamide Antimalarials with Mammalian Protein Farnesyltransferase Inhibitory Activity</title><author>Ryckebusch, Adina ; Gilleron, Pauline ; Millet, Régis ; Houssin, Raymond ; Lemoine, Amélie ; Pommery, Nicole ; Grellier, Philippe ; Sergheraert, Christian ; Hénichart, Jean-Pierre</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c536t-d094fb6ac50e5fda9044a7bb87125a5875bf1a512724b3bc58ad359ec55315c33</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2005</creationdate><topic>Alkyl and Aryl Transferases - antagonists & inhibitors</topic><topic>Animals</topic><topic>Antimalarials - chemical synthesis</topic><topic>Antimalarials - chemistry</topic><topic>Antimalarials - pharmacology</topic><topic>Benzamides - chemical synthesis</topic><topic>Benzamides - chemistry</topic><topic>Benzamides - pharmacology</topic><topic>Cell Line, Tumor</topic><topic>Cell Proliferation - drug effects</topic><topic>Chemical Sciences</topic><topic>Drug Design</topic><topic>Drug Evaluation, Preclinical</topic><topic>Drug Screening Assays, Antitumor</topic><topic>farnesyltransferase</topic><topic>Humans</topic><topic>inhibitor</topic><topic>Life Sciences</topic><topic>malaria</topic><topic>Mice</topic><topic>Microbiology and Parasitology</topic><topic>Molecular Structure</topic><topic>N-(4-piperidinyl)benzamide derivative</topic><topic>Parasitic Sensitivity Tests</topic><topic>Plasmodium falciparum</topic><topic>Plasmodium falciparum - drug effects</topic><topic>Plasmodium falciparum - enzymology</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ryckebusch, Adina</creatorcontrib><creatorcontrib>Gilleron, Pauline</creatorcontrib><creatorcontrib>Millet, Régis</creatorcontrib><creatorcontrib>Houssin, Raymond</creatorcontrib><creatorcontrib>Lemoine, Amélie</creatorcontrib><creatorcontrib>Pommery, Nicole</creatorcontrib><creatorcontrib>Grellier, Philippe</creatorcontrib><creatorcontrib>Sergheraert, Christian</creatorcontrib><creatorcontrib>Hénichart, Jean-Pierre</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Neurosciences Abstracts</collection><collection>Nucleic Acids Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>MEDLINE - Academic</collection><collection>Hyper Article en Ligne (HAL)</collection><collection>Hyper Article en Ligne (HAL) (Open Access)</collection><jtitle>Chemical & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ryckebusch, Adina</au><au>Gilleron, Pauline</au><au>Millet, Régis</au><au>Houssin, Raymond</au><au>Lemoine, Amélie</au><au>Pommery, Nicole</au><au>Grellier, Philippe</au><au>Sergheraert, Christian</au><au>Hénichart, Jean-Pierre</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel N-(4-Piperidinyl)benzamide Antimalarials with Mammalian Protein Farnesyltransferase Inhibitory Activity</atitle><jtitle>Chemical & pharmaceutical bulletin</jtitle><addtitle>Chem. Pharm. Bull.</addtitle><date>2005-10-01</date><risdate>2005</risdate><volume>53</volume><issue>10</issue><spage>1324</spage><epage>1326</epage><pages>1324-1326</pages><issn>0009-2363</issn><eissn>1347-5223</eissn><abstract>Protein farnesyltransferase of Plasmodium falciparum is a potential target in the treatment of malaria for which increased drug resistance is observed. The design, synthesis and evaluation of a series of N-(4-piperidinyl)benzamides is reported. The most potent compounds showed in vitro activity against the parasite at submicromolar concentrations.</abstract><cop>Japan</cop><pub>The Pharmaceutical Society of Japan</pub><pmid>16204993</pmid><doi>10.1248/cpb.53.1324</doi><tpages>3</tpages><orcidid>https://orcid.org/0000-0003-4153-0465</orcidid><oa>free_for_read</oa></addata></record> |
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| language | eng |
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| source | J-STAGE Free; MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Free Full-Text Journals in Chemistry |
| subjects | Alkyl and Aryl Transferases - antagonists & inhibitors Animals Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - pharmacology Benzamides - chemical synthesis Benzamides - chemistry Benzamides - pharmacology Cell Line, Tumor Cell Proliferation - drug effects Chemical Sciences Drug Design Drug Evaluation, Preclinical Drug Screening Assays, Antitumor farnesyltransferase Humans inhibitor Life Sciences malaria Mice Microbiology and Parasitology Molecular Structure N-(4-piperidinyl)benzamide derivative Parasitic Sensitivity Tests Plasmodium falciparum Plasmodium falciparum - drug effects Plasmodium falciparum - enzymology Structure-Activity Relationship |
| title | Novel N-(4-Piperidinyl)benzamide Antimalarials with Mammalian Protein Farnesyltransferase Inhibitory Activity |
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