Synthesis and antifilarial evaluation of 7-O-acetamidyl-4-alkyl-2H-1-benzopyran-2-ones.


A series of 7-O-acetamidyl-4-alkyl-2H-1-benzopyran-2-ones (5-23) has been synthesized by amidation of 7-O-(carbethoxymethyl)-4-alkyl-2H-1-benzopyran-2-ones (2a, 2b) with different primary and secondary amines in fair to good yield. The resulting compounds were screened for their filarial DNA topoisomerase inhibitory activity under in vivo condition in Setaria cervi. The compounds were tested in vitro against Brugia malayi. A few of the compounds possess promising antifilarial activity.


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@article{Katiyar2003SynthesisAA, title={Synthesis and antifilarial evaluation of 7-O-acetamidyl-4-alkyl-2H-1-benzopyran-2-ones.}, author={Diksha Katiyar and Vinod Kumar Tiwari and Rama Pati Tripathi and Velurijagan Mohan Reddy and Shailza Mishra Bhattacharya and Jitendra Kumar Saxena}, journal={Arzneimittel-Forschung}, year={2003}, volume={53 12}, pages={857-63} }