New antiprotozoal agents: Synthesis and biological evaluation of different 4-(7-chloroquinolin-4-yl) piperazin-1-yl)pyrrolidin-2-yl) methanone derivatives
- Authors
- Ansari, Mohammad Fawad; Hayat, Faisal; Inam, Afreen; Kathrada, Fatima; van Zyl, Robyn L.; Coetzee, Maureen; Ahmad, Kamal; Shin, Dongyun; Azam, Amir
- Issue Date
- 1-Feb-2017
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Metronidazole; Amoebiasis; Entamoeba histolytic; Plasmodium falciparum; MIT-assay; Thioredoxin reductase
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.27, no.3, pp.460 - 465
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 27
- Number
- 3
- Start Page
- 460
- End Page
- 465
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/6404
- DOI
- 10.1016/j.bmcl.2016.12.043
- ISSN
- 0960-894X
- 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.
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