Pentavalent Antimonials: New Perspectives for Old Drugs

Pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate, have been used for more than half a century in the therapy of the parasitic disease leishmaniasis. Even though antimonials are still the first-line drugs, they exhibit several limitations, including severe side effec...
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Autor*in:	Raul R. Ribeiro [verfasserIn] Cynthia Demicheli [verfasserIn] Frédéric Frézard [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2009

Schlagwörter:	pentavalent antimonials meglumine antimoniate cyclodextrin liposomes leishmaniasis

Übergeordnetes Werk:	In: Molecules - MDPI AG, 2003, 14(2009), 7, Seite 2317-2336
Übergeordnetes Werk:	volume:14 ; year:2009 ; number:7 ; pages:2317-2336

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.3390/molecules14072317

Katalog-ID:	DOAJ037202669

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520			\|a Pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate, have been used for more than half a century in the therapy of the parasitic disease leishmaniasis. Even though antimonials are still the first-line drugs, they exhibit several limitations, including severe side effects, the need for daily parenteral administration and drug resistance. The molecular structure of antimonials, their metabolism and mechanism of action are still being investigated. Some recent studies suggest that pentavalent antimony acts as a prodrug that is converted to active and more toxic trivalent antimony. Other works support the direct involvement of pentavalent antimony. Recent data suggest that the biomolecules, thiols and ribonucleosides, may mediate the actions of these drugs. This review will summarize the progress to date on the chemistry and biochemistry of pentavalent antimony. It will also present the most recent works being done to improve antimonial chemotherapy. These works include the development of simple synthetic methods for pentavalent antimonials, liposome-based formulations for targeting the Leishmania parasites responsible for visceral leishmaniasis and cyclodextrin-based formulations to promote the oral delivery of antimony.
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allfields	10.3390/molecules14072317 doi (DE-627)DOAJ037202669 (DE-599)DOAJ478dfbd0521847c6a909323186c63853 DE-627 ger DE-627 rakwb eng QD241-441 Raul R. Ribeiro verfasserin aut Pentavalent Antimonials: New Perspectives for Old Drugs 2009 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate, have been used for more than half a century in the therapy of the parasitic disease leishmaniasis. Even though antimonials are still the first-line drugs, they exhibit several limitations, including severe side effects, the need for daily parenteral administration and drug resistance. The molecular structure of antimonials, their metabolism and mechanism of action are still being investigated. Some recent studies suggest that pentavalent antimony acts as a prodrug that is converted to active and more toxic trivalent antimony. Other works support the direct involvement of pentavalent antimony. Recent data suggest that the biomolecules, thiols and ribonucleosides, may mediate the actions of these drugs. This review will summarize the progress to date on the chemistry and biochemistry of pentavalent antimony. It will also present the most recent works being done to improve antimonial chemotherapy. These works include the development of simple synthetic methods for pentavalent antimonials, liposome-based formulations for targeting the Leishmania parasites responsible for visceral leishmaniasis and cyclodextrin-based formulations to promote the oral delivery of antimony. pentavalent antimonials meglumine antimoniate cyclodextrin liposomes leishmaniasis Organic chemistry Cynthia Demicheli verfasserin aut Frédéric Frézard verfasserin aut In Molecules MDPI AG, 2003 14(2009), 7, Seite 2317-2336 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:14 year:2009 number:7 pages:2317-2336 https://doi.org/10.3390/molecules14072317 kostenfrei https://doaj.org/article/478dfbd0521847c6a909323186c63853 kostenfrei http://www.mdpi.com/1420-3049/14/7/2317/ kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 14 2009 7 2317-2336
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allfieldsSound	10.3390/molecules14072317 doi (DE-627)DOAJ037202669 (DE-599)DOAJ478dfbd0521847c6a909323186c63853 DE-627 ger DE-627 rakwb eng QD241-441 Raul R. Ribeiro verfasserin aut Pentavalent Antimonials: New Perspectives for Old Drugs 2009 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate, have been used for more than half a century in the therapy of the parasitic disease leishmaniasis. Even though antimonials are still the first-line drugs, they exhibit several limitations, including severe side effects, the need for daily parenteral administration and drug resistance. The molecular structure of antimonials, their metabolism and mechanism of action are still being investigated. Some recent studies suggest that pentavalent antimony acts as a prodrug that is converted to active and more toxic trivalent antimony. Other works support the direct involvement of pentavalent antimony. Recent data suggest that the biomolecules, thiols and ribonucleosides, may mediate the actions of these drugs. This review will summarize the progress to date on the chemistry and biochemistry of pentavalent antimony. It will also present the most recent works being done to improve antimonial chemotherapy. These works include the development of simple synthetic methods for pentavalent antimonials, liposome-based formulations for targeting the Leishmania parasites responsible for visceral leishmaniasis and cyclodextrin-based formulations to promote the oral delivery of antimony. pentavalent antimonials meglumine antimoniate cyclodextrin liposomes leishmaniasis Organic chemistry Cynthia Demicheli verfasserin aut Frédéric Frézard verfasserin aut In Molecules MDPI AG, 2003 14(2009), 7, Seite 2317-2336 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:14 year:2009 number:7 pages:2317-2336 https://doi.org/10.3390/molecules14072317 kostenfrei https://doaj.org/article/478dfbd0521847c6a909323186c63853 kostenfrei http://www.mdpi.com/1420-3049/14/7/2317/ kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 14 2009 7 2317-2336
language	English
source	In Molecules 14(2009), 7, Seite 2317-2336 volume:14 year:2009 number:7 pages:2317-2336
sourceStr	In Molecules 14(2009), 7, Seite 2317-2336 volume:14 year:2009 number:7 pages:2317-2336
format_phy_str_mv	Article
institution	findex.gbv.de
topic_facet	pentavalent antimonials meglumine antimoniate cyclodextrin liposomes leishmaniasis Organic chemistry
isfreeaccess_bool	true
container_title	Molecules
authorswithroles_txt_mv	Raul R. Ribeiro @@aut@@ Cynthia Demicheli @@aut@@ Frédéric Frézard @@aut@@
publishDateDaySort_date	2009-01-01T00:00:00Z
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callnumber-first	Q - Science
author	Raul R. Ribeiro
spellingShingle	Raul R. Ribeiro misc QD241-441 misc pentavalent antimonials misc meglumine antimoniate misc cyclodextrin misc liposomes misc leishmaniasis misc Organic chemistry Pentavalent Antimonials: New Perspectives for Old Drugs
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topic_title	QD241-441 Pentavalent Antimonials: New Perspectives for Old Drugs pentavalent antimonials meglumine antimoniate cyclodextrin liposomes leishmaniasis
topic	misc QD241-441 misc pentavalent antimonials misc meglumine antimoniate misc cyclodextrin misc liposomes misc leishmaniasis misc Organic chemistry
topic_unstemmed	misc QD241-441 misc pentavalent antimonials misc meglumine antimoniate misc cyclodextrin misc liposomes misc leishmaniasis misc Organic chemistry
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title	Pentavalent Antimonials: New Perspectives for Old Drugs
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title_sort	pentavalent antimonials: new perspectives for old drugs
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title_auth	Pentavalent Antimonials: New Perspectives for Old Drugs
abstract	Pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate, have been used for more than half a century in the therapy of the parasitic disease leishmaniasis. Even though antimonials are still the first-line drugs, they exhibit several limitations, including severe side effects, the need for daily parenteral administration and drug resistance. The molecular structure of antimonials, their metabolism and mechanism of action are still being investigated. Some recent studies suggest that pentavalent antimony acts as a prodrug that is converted to active and more toxic trivalent antimony. Other works support the direct involvement of pentavalent antimony. Recent data suggest that the biomolecules, thiols and ribonucleosides, may mediate the actions of these drugs. This review will summarize the progress to date on the chemistry and biochemistry of pentavalent antimony. It will also present the most recent works being done to improve antimonial chemotherapy. These works include the development of simple synthetic methods for pentavalent antimonials, liposome-based formulations for targeting the Leishmania parasites responsible for visceral leishmaniasis and cyclodextrin-based formulations to promote the oral delivery of antimony.
abstractGer	Pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate, have been used for more than half a century in the therapy of the parasitic disease leishmaniasis. Even though antimonials are still the first-line drugs, they exhibit several limitations, including severe side effects, the need for daily parenteral administration and drug resistance. The molecular structure of antimonials, their metabolism and mechanism of action are still being investigated. Some recent studies suggest that pentavalent antimony acts as a prodrug that is converted to active and more toxic trivalent antimony. Other works support the direct involvement of pentavalent antimony. Recent data suggest that the biomolecules, thiols and ribonucleosides, may mediate the actions of these drugs. This review will summarize the progress to date on the chemistry and biochemistry of pentavalent antimony. It will also present the most recent works being done to improve antimonial chemotherapy. These works include the development of simple synthetic methods for pentavalent antimonials, liposome-based formulations for targeting the Leishmania parasites responsible for visceral leishmaniasis and cyclodextrin-based formulations to promote the oral delivery of antimony.
abstract_unstemmed	Pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate, have been used for more than half a century in the therapy of the parasitic disease leishmaniasis. Even though antimonials are still the first-line drugs, they exhibit several limitations, including severe side effects, the need for daily parenteral administration and drug resistance. The molecular structure of antimonials, their metabolism and mechanism of action are still being investigated. Some recent studies suggest that pentavalent antimony acts as a prodrug that is converted to active and more toxic trivalent antimony. Other works support the direct involvement of pentavalent antimony. Recent data suggest that the biomolecules, thiols and ribonucleosides, may mediate the actions of these drugs. This review will summarize the progress to date on the chemistry and biochemistry of pentavalent antimony. It will also present the most recent works being done to improve antimonial chemotherapy. These works include the development of simple synthetic methods for pentavalent antimonials, liposome-based formulations for targeting the Leishmania parasites responsible for visceral leishmaniasis and cyclodextrin-based formulations to promote the oral delivery of antimony.
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title_short	Pentavalent Antimonials: New Perspectives for Old Drugs
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