Sulfonamide chalcones: Synthesis and in vitro exploration for therapeutic potential against Brugia malayi.
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.
Department of Chemistry, G. S. Science, Arts and Commerce College, Khamgaon 444303, India.
Sandeep P
SP
Bahekar
Department of Biochemistry, Mahatma Gandhi Institute of Medical Sciences and JB Tropical Disease Research Centre, Sevagram, Wardha 442102, India.
Sneha V
SV
Hande
Department of Chemistry, G. S. Science, Arts and Commerce College, Khamgaon 444303, India.
Nikita R
NR
Agrawal
Department of Chemistry, G. S. Science, Arts and Commerce College, Khamgaon 444303, India. Electronic address: chemants@gmail.com.
Hemant S
HS
Chandak
Department of Biochemistry, Mahatma Gandhi Institute of Medical Sciences and JB Tropical Disease Research Centre, Sevagram, Wardha 442102, India.
Priyanka S
PS
Bhoj
Department of Biochemistry, Mahatma Gandhi Institute of Medical Sciences and JB Tropical Disease Research Centre, Sevagram, Wardha 442102, India. Electronic address: goswamikln@gmail.com.
Kalyan
K
Goswami
Department of Biochemistry, Mahatma Gandhi Institute of Medical Sciences and JB Tropical Disease Research Centre, Sevagram, Wardha 442102, India.
M V R
MVR
Reddy
D000818:Animals; D017178:Brugia malayi / Q000187:drug effects* / Q000254:growth & development; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D005369:Filaricides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D020128:Inhibitory Concentration 50; D008018:Life Cycle Stages; D008958:Models, Molecular; D008968:Molecular Conformation
D047188:Chalcones; D005369:Filaricides
Antifilarial; Brugia malayi; Claisen-Schimdt condensation; Sulfonamide chalcone