Synthesis, anti-plasmodial and cytotoxic evaluation of 1H-1, 2, 3-triazole/acyl hydrazide integrated tetrahydro-β-carboline-4-aminoquinoline conjugates. Issue 2 (15th January 2020)

• Record Type: Journal Article
• Authors: Sharma, Bharvi; Kaur, Simranjeet; Legac, Jenny; Rosenthal, Philip J.; Kumar, Vipan
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 30:Issue 2(2020)
• Publication Date: 2020-01-15
• Subjects: Tetrahydro-β-carboline -- Quinoline -- Triazole -- Acyl hydrazide -- Antiplasmodial; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2019.126810
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of 1 H -1, 2, 3-triazole/acylhydrazide-tethered tetrahydro- β -carboline-4-aminoquinoline conjugates was synthesized with an aim to study their anti-plasmodial structure-activity relationship. The presence of 1 H -1, 2, 3-triazole-core along with a flexible alkyl chain length on aminoquinoline core has favourable influence on the anti-plasmodial activity against Chloroquine-resistant W2 strain of P. falciparum while the introduction of hydrazine core not only diminished the activities but also resulted in increased cytotoxicity against mammalian Vero cells.