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Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives |
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| Authors: | Singh Pardeep Sachdeva Shaveta Raj Raghu Kumar Vipan Mahajan Mohinder P Nasser Shereen Vivas Livia Gut Jiri Rosenthal Phillip J Feng Tzu-Shean Chibale Kelly |
| Institution: | a Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India b London School of Hygiene and Tropical Medicine, Keppel Street, London, UK c Department of Medicine, San Francisco General Hospital, CA 94143, USA d Department of Chemistry and Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Private Bag, Rondebosch 7701, South Africa |
| Abstract: | 3-Azido-, 3-amino- and 3-(1,2,3-triazol-1-yl)-β-lactams were synthesized and evaluated for their antiplasmodial activity against four strains of Plasmodium falciparum and KB cells for their cytotoxicity profiles. The presence of a cyclohexyl substituent at N-1 and a phenyl group on the triazole ring markedly improved the activity profiles of triazole-tethered β-lactam exhibiting IC50 values of 1.13, 1.21 and 1.00 μM against 3D7, K1 and W2 strains respectively. |
| Keywords: | c-3 Functionalized b-lactams Triazoles Click chemistry Antiplasmodial evaluation |
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