Document Report Card

Basic Information

ID: ALA3870323

Journal: Eur J Med Chem

Title: Sulfonamide chalcones: Synthesis and in vitro exploration for therapeutic potential against Brugia malayi.

Authors: Bahekar SP, Hande SV, Agrawal NR, Chandak HS, Bhoj PS, Goswami K, Reddy MVR.

Abstract: Keeping in mind the immense biological potential of chalcones and sulfonamide scaffolds, a library of sulfonamide chalcones has been synthesized and evaluated for in vitro antifilarial assay against human lymphatic filarial parasite Brugia malayi. Experimental evidence showcased for the first time the potential of some sulfonamide chalcones as effective and safe antifilarial lead molecules against human lymphatic filarial parasite B. malayi. Sulfonamide chalcones 4d, 4p, 4q, 4t and 4aa displayed the significantly wide therapeutic window. Particularly chalcones with halogen substitution in aromatic ring proved to be potent antifilarial agents against Brugia malayi. Sulphonamide chalcones with lipophilic methyl moiety (4q and 4aa) at para position of terminal phenyl rings of compounds were found to have remarkable antifilarial activities with therapeutic efficacy. Observed preliminary evidence of apoptosis by effective chalcone derivatives envisaged its fair possibility to inhibit folate pathway with consequent defect in DNA synthesis.

CiteXplore: 27592395

DOI: 10.1016/j.ejmech.2016.08.042