Evaluation of vanillic acid analogues as a new class of antifilarial agents.
A number of vanillic acid analogues (1-14) have been synthesised and evaluated against experimental filarial infections using cotton rats (Sigmodon hispidus) infected with Litomosoides carinii, a primary screening model, at a dose of 30 mg/kg, ip for 5 days. Of the 8 compounds tested, 4 (5,7, 11 and 12) exhibited high micro- and macro-filaricidal activity with sterilization of surviving female worms. Compounds 5, 7, 12 showed remarkable adulticidal action (> 80%). Sterilization of the female worms by compounds 11 and 12 was highly significant (80-100%).
Varma
R S
RS
Department of Chemistry, Lucknow University, India.
Shukla
A
A
Chatterjee
R K
RK
D000818:Animals; D004353:Drug Evaluation, Preclinical; D005260:Female; D005369:Filaricides / Q000737:chemistry / Q000494:pharmacology*; D005370:Filarioidea / Q000187:drug effects*; D008297:Male; D016205:Sigmodontinae; D014641:Vanillic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology
D005369:Filaricides; D014641:Vanillic Acid