Targeting Asexual and Sexual Blood Stages of the Human Malaria Parasite P. falciparum with 7‐Chloroquinoline‐Based 1,2,3‐Triazoles

• DOI: 10.1002/cmdc.201800728
• Publication Date: 2019-01-04T19:27:29Z
• Authors: Ishan Wadi; Davinder Prasad; Neha Batra; Kumkum Srivastava; Anupkumar R. Anvikar; Neena Valecha; Mahendra Nath
• Keywords: Strain (injury)

Abstract Novel 4‐amino‐7‐chloroquinoline‐based 1,2,3‐triazole hybrids were synthesised in good yields by Cu I ‐catalysed Huisgen 1,3‐dipolar cycloaddition reactions of 2‐azido‐ N ‐(7‐chloroquinolin‐4‐ylaminoalkyl)acetamides with various terminal alkynes. These new screened vitro against asexual blood stages the chloroquine‐sensitive 3D7 strain P. falciparum . The most active compounds further and sexual (gametocytes) chloroquine‐resistant RKL‐9 Although all less potent than chloroquine strain, three best appreciably more displaying IC 50 values <100 n m , one them having an 2.94 Further, lead gametocytocidal micromolar range, observed to induce morphological deformations mature gametocytes. Most demonstrated little or no cytotoxicity exhibited selectivity indices. represent promising candidates for evaluation their schizonticidal potential.