The new pyrazolyltetrazole derivative MSN20 is effective via oral delivery against cutaneous leishmaniasis
An orally delivered, safe and effective treatment for leishmaniasis is an unmet medical need. Azoles and the pyrazolylpyrimidine allopurinol present leishmanicidal activity, but their clinical efficacies are variable. Here, we describe the activity of the new pyrazolyltetrazole hybrid, 5-[5-amino-1-...
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| Veröffentlicht in: | Antimicrobial agents and chemotherapy 2014-10, Vol.58 (10), p.6290-6293 |
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| container_title | Antimicrobial agents and chemotherapy |
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| creator | Faiões, Viviane Dos Santos Dos Santos, Maurício Silva Bernardino, Alice Maria Rolim Cunha-Júnior, Edézio Ferreira Canto Cavalheiro, Marilene Marcuzzo do Torres-Santos, Eduardo Caio |
| description | An orally delivered, safe and effective treatment for leishmaniasis is an unmet medical need. Azoles and the pyrazolylpyrimidine allopurinol present leishmanicidal activity, but their clinical efficacies are variable. Here, we describe the activity of the new pyrazolyltetrazole hybrid, 5-[5-amino-1-(4'-methoxyphenyl)1H-pyrazole-4-yl]1H-tetrazole (MSN20). MSN20 showed a 50% inhibitory concentration (IC50) of 22.3 μM against amastigotes of Leishmania amazonensis and reduced significantly the parasite load in infected mice, suggesting its utility as a lead compound for the development of an oral treatment for leishmaniasis. |
| doi_str_mv | 10.1128/AAC.02874-14 |
| format | Article |
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All Rights Reserved.</rights><rights>Copyright © 2014, American Society for Microbiology. All Rights Reserved. 2014 American Society for Microbiology</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-a451t-9ed68947ae3f252fc8ed7476ec1e946ddd09974e4c85936266d18054f6de9e063</citedby><cites>FETCH-LOGICAL-a451t-9ed68947ae3f252fc8ed7476ec1e946ddd09974e4c85936266d18054f6de9e063</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4187983/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4187983/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,723,776,780,881,27901,27902,53766,53768</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/25092697$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Faiões, Viviane Dos Santos</creatorcontrib><creatorcontrib>Dos Santos, Maurício Silva</creatorcontrib><creatorcontrib>Bernardino, Alice Maria Rolim</creatorcontrib><creatorcontrib>Cunha-Júnior, Edézio Ferreira</creatorcontrib><creatorcontrib>Canto Cavalheiro, Marilene Marcuzzo do</creatorcontrib><creatorcontrib>Torres-Santos, Eduardo Caio</creatorcontrib><title>The new pyrazolyltetrazole derivative MSN20 is effective via oral delivery against cutaneous leishmaniasis</title><title>Antimicrobial agents and chemotherapy</title><addtitle>Antimicrob Agents Chemother</addtitle><addtitle>Antimicrob Agents Chemother</addtitle><description>An orally delivered, safe and effective treatment for leishmaniasis is an unmet medical need. 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MSN20 showed a 50% inhibitory concentration (IC50) of 22.3 μM against amastigotes of Leishmania amazonensis and reduced significantly the parasite load in infected mice, suggesting its utility as a lead compound for the development of an oral treatment for leishmaniasis.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Antiprotozoal Agents</subject><subject>Antiprotozoal Agents - administration & dosage</subject><subject>Antiprotozoal Agents - chemistry</subject><subject>Antiprotozoal Agents - pharmacology</subject><subject>Experimental Therapeutics</subject><subject>Inhibitory Concentration 50</subject><subject>Leishmania amazonensis</subject><subject>Leishmaniasis, Cutaneous</subject><subject>Leishmaniasis, Cutaneous - drug therapy</subject><subject>Mice</subject><subject>Pyrazoles</subject><subject>Pyrazoles - chemistry</subject><subject>Structure-Activity Relationship</subject><subject>Tetrazoles</subject><subject>Tetrazoles - chemistry</subject><issn>0066-4804</issn><issn>1098-6596</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kcFv2yAYxVHVakmz3XquOLbS3AHGGC6ToqjrJmXrodkZUfM5IcJ2Bnam9K8vS7qoPfQE7-On9-nxELqg5IZSJr9Mp7MbwmTJM8pP0JgSJTNRKHGKxoQIkXFJ-Aidx7gmSReKfEAjVhDFhCrHaL1YAW7hL97sgnnq_M730O9vgC0EtzW92wL--fCLEewihrqGaj_aOoO7YHzCfNJhh83SuDb2uBp600I3ROzBxVVjWmeiix_RWW18hE8v5wT9_na7mH3P5vd3P2bTeWZ4QftMgRVS8dJAXrOC1ZUEW_JSQEVBcWGtJUqVHHglC5ULJoSlkhS8FhYUEJFP0NeD72Z4bMBW0KZAXm-Ca0zY6c44_faldSu97LaaU1kqmSeDqxeD0P0ZIPa6cbEC7w-pNBWMCUJKyhL6-YBWoYsxQH1cQ4n-V49O9eh9PZryhF8fcBMbptfdENr0E--xl69jHI3_d5c_A7nUmfY</recordid><startdate>20141001</startdate><enddate>20141001</enddate><creator>Faiões, Viviane Dos Santos</creator><creator>Dos Santos, Maurício Silva</creator><creator>Bernardino, Alice Maria Rolim</creator><creator>Cunha-Júnior, Edézio Ferreira</creator><creator>Canto Cavalheiro, Marilene Marcuzzo do</creator><creator>Torres-Santos, Eduardo Caio</creator><general>American Society for Microbiology</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>7T7</scope><scope>8FD</scope><scope>C1K</scope><scope>F1W</scope><scope>FR3</scope><scope>H95</scope><scope>H97</scope><scope>L.G</scope><scope>M7N</scope><scope>P64</scope><scope>5PM</scope></search><sort><creationdate>20141001</creationdate><title>The new pyrazolyltetrazole derivative MSN20 is effective via oral delivery against cutaneous leishmaniasis</title><author>Faiões, Viviane Dos Santos ; 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| ispartof | Antimicrobial agents and chemotherapy, 2014-10, Vol.58 (10), p.6290-6293 |
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| source | MEDLINE; EZB-FREE-00999 freely available EZB journals; PubMed Central |
| subjects | Administration, Oral Animals Antiprotozoal Agents Antiprotozoal Agents - administration & dosage Antiprotozoal Agents - chemistry Antiprotozoal Agents - pharmacology Experimental Therapeutics Inhibitory Concentration 50 Leishmania amazonensis Leishmaniasis, Cutaneous Leishmaniasis, Cutaneous - drug therapy Mice Pyrazoles Pyrazoles - chemistry Structure-Activity Relationship Tetrazoles Tetrazoles - chemistry |
| title | The new pyrazolyltetrazole derivative MSN20 is effective via oral delivery against cutaneous leishmaniasis |
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