title: Synthesis and antifilarial evaluation of 7-O-acetamidyl-4-alkyl-2H-1-benzopyran-2-ones.
abstract: 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.
authors.affiliation: Medicinal Chemistry Division, Central Drug Research Institute, Lucknow, India.
authors.forename: Diksha
authors.initials: D
authors.lastname: Katiyar
authors.forename: Vinod Kumar
authors.initials: VK
authors.lastname: Tiwari
authors.forename: Rama Pati
authors.initials: RP
authors.lastname: Tripathi
authors.forename: Velurijagan Mohan
authors.initials: VM
authors.lastname: Reddy
authors.forename: Shailza Mishra
authors.initials: SM
authors.lastname: Bhattacharya
authors.forename: Jitendra Kumar
authors.initials: JK
authors.lastname: Saxena
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis* / Q000627:therapeutic use*; D000818:Animals; D001578:Benzopyrans / Q000138:chemical synthesis* / Q000627:therapeutic use*; D017178:Brugia malayi / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005260:Female; D005369:Filaricides / Q000138:chemical synthesis* / Q000627:therapeutic use*; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D017182:Setaria Nematode / Q000187:drug effects; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
chemical_list: D000081:Acetamides; D001578:Benzopyrans; D004791:Enzyme Inhibitors; D005369:Filaricides; D007202:Indicators and Reagents; D059005:Topoisomerase II Inhibitors