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New antiprotozoal agents: Synthesis and biological evaluation of different 4-(7-chloroquinolin-4-yl) piperazin-1-yl)pyrrolidin-2-yl)methanone derivatives |
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| Authors: | Mohammad Fawad Ansari Faisal Hayat Afreen Inam Fatima Kathrada Robyn L. van Zyl Maureen Coetzee Kamal Ahmad Dongyun Shin Amir Azam |
| Affiliation: | 1. Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India;2. College of Pharmacy, Gachon University, 191 Hambakmoe-ro, Yeonsu-gu, Incheon 406-799, South Korea;3. Pharmacology Division, Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of Witwatersrand, Johannesburg 2193, South Africa;4. WITS Research Institute for Malaria (WRIM), Faculty of Health Sciences, University of Witwatersrand, Johannesburg 2193, South Africa;5. Vector Control Reference Unit, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg, South Africa;6. Centre for Interdisciplinary Science, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India |
| 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 μM) lower than the standard drug metronidazole (IC50 1.80 μM). All nine compounds exhibited antimalarial activity (IC50 range: 1.42–19.62 μM), 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 μM) than quinine (IC50: 275.6 ± 16.46 μM) against the human kidney epithelial cells. None of the compounds exhibited any inhibitory effect on the viability of Anopheles arabiensis mosquito larvae. |
| Keywords: | Metronidazole Amoebiasis MTT-assay Thioredoxin reductase |
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