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

被引：53

作者：

Bahekar, Sandeep P. ^{[1
]}

Hande, Sneha V. ^{[2
,3
]}

Agrawal, Nikita R. ^{[1
]}

Chandak, Hemant S. ^{[1
]}

Bhoj, Priyanka S. ^{[2
,3
]}

Goswami, Kalyan ^{[2
,3
]}

Reddy, M. V. R. ^{[2
,3
]}

机构：

[1] GS Sci Arts & Commerce Coll, Dept Chem, Khamgaon 444303, India

[2] Mahatma Gandhi Inst Med Sci, Dept Biochem, Sevagram 442102, Wardha, India

[3] JB Trop Dis Res Ctr, Sevagram 442102, Wardha, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 124卷

关键词：

Sulfonamide chalcone; Antifilarial; Claisen-Schimdt condensation; Brugia malayi; BIOLOGICAL EVALUATION; PLASMODIUM-FALCIPARUM; ANTIMALARIAL ACTIVITY; LICOCHALCONE-A; INHIBITORS; DERIVATIVES; ANTICANCER; AGENTS; MICROFILARIAE; GLUTATHIONE;

D O I：

10.1016/j.ejmech.2016.08.042

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2016 Elsevier Masson SAS. All rights reserved.

引用

页码：262 / 269

页数：8

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