New antiprotozoal agents: Synthesis and biological evaluation of different 4-(7-chloroquinolin-4-yl) piperazin-1-yl)pyrrolidin-2-yl) methanone derivatives
DC Field | Value | Language |
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dc.contributor.author | Ansari, Mohammad Fawad | - |
dc.contributor.author | Hayat, Faisal | - |
dc.contributor.author | Inam, Afreen | - |
dc.contributor.author | Kathrada, Fatima | - |
dc.contributor.author | van Zyl, Robyn L. | - |
dc.contributor.author | Coetzee, Maureen | - |
dc.contributor.author | Ahmad, Kamal | - |
dc.contributor.author | Shin, Dongyun | - |
dc.contributor.author | Azam, Amir | - |
dc.date.available | 2020-02-27T19:43:40Z | - |
dc.date.created | 2020-02-07 | - |
dc.date.issued | 2017-02-01 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/6404 | - |
dc.description.abstract | In an endeavor to develop efficacious antiprotozoal agents 4-(7-chloroquinolin-4-yl) piperazin-1-yl) pyrrolidin-2-yl)methanone derivatives (5-14) were synthesized, characterized and biologically evaluated for antiprotozoal activity. The compounds were screened in vitro against the HM1: IMSS strain of Entamoeba histolytica and NF54 chloroquine-sensitive strain of Plasmodium falciparum. Among the synthesized compounds six exhibited promising antiamoebic activity with IC50 values (0.14-1.26 mu M) lower than the standard drug metronidazole (IC50 1.80 mu M). All nine compounds exhibited antimalarial activity (IC50 range: 1.42-19.62 mu M), while maintaining a favorable safety profile to host red blood cells. All the compounds were less effective as an antimalarial and more toxic (IC50 range: 14.67-81.24 mu M) than quinine (IC50: 275.6 +/- 16.46 mu M) against the human kidney epithelial cells. None of the compounds exhibited any inhibitory effect on the viability of Anopheles arabiensis mosquito larvae. (C) 2016 Elsevier Ltd. All rights reserved. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.subject | BETA-HEMATIN FORMATION | - |
dc.subject | ANTIAMEBIC ACTIVITY | - |
dc.subject | MOLECULAR DOCKING | - |
dc.subject | DESIGN | - |
dc.subject | MALARIA | - |
dc.subject | HYBRIDS | - |
dc.subject | INHIBITION | - |
dc.subject | RESISTANCE | - |
dc.subject | AMEBIASIS | - |
dc.subject | AMINO | - |
dc.title | New antiprotozoal agents: Synthesis and biological evaluation of different 4-(7-chloroquinolin-4-yl) piperazin-1-yl)pyrrolidin-2-yl) methanone derivatives | - |
dc.type | Article | - |
dc.type.rims | ART | - |
dc.description.journalClass | 1 | - |
dc.identifier.wosid | 000392900600017 | - |
dc.identifier.doi | 10.1016/j.bmcl.2016.12.043 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.27, no.3, pp.460 - 465 | - |
dc.identifier.scopusid | 2-s2.0-85008194166 | - |
dc.citation.endPage | 465 | - |
dc.citation.startPage | 460 | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.volume | 27 | - |
dc.citation.number | 3 | - |
dc.contributor.affiliatedAuthor | Hayat, Faisal | - |
dc.contributor.affiliatedAuthor | Shin, Dongyun | - |
dc.type.docType | Article | - |
dc.subject.keywordAuthor | Metronidazole | - |
dc.subject.keywordAuthor | Amoebiasis | - |
dc.subject.keywordAuthor | Entamoeba histolytic | - |
dc.subject.keywordAuthor | Plasmodium falciparum | - |
dc.subject.keywordAuthor | MIT-assay | - |
dc.subject.keywordAuthor | Thioredoxin reductase | - |
dc.subject.keywordPlus | BETA-HEMATIN FORMATION | - |
dc.subject.keywordPlus | ANTIAMEBIC ACTIVITY | - |
dc.subject.keywordPlus | MOLECULAR DOCKING | - |
dc.subject.keywordPlus | DESIGN | - |
dc.subject.keywordPlus | MALARIA | - |
dc.subject.keywordPlus | HYBRIDS | - |
dc.subject.keywordPlus | INHIBITION | - |
dc.subject.keywordPlus | RESISTANCE | - |
dc.subject.keywordPlus | AMEBIASIS | - |
dc.subject.keywordPlus | AMINO | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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