Antileishmanial assessment of isoxazole derivatives against <i>L. donovani</i>

Abstract

A chemical library comprising substituted 3-nitroisoxazoles and 3-aminoisoxazoles was prepared and screened for their antileishmanial activity against <i>L. donovani</i>. As compared to Miltefosine, the standard drug used in bioassays, several compounds displayed remarkably better inhibition of the promastigote and amastigote stages of parasites. The <i>in vivo</i> evaluation of a few compounds in a golden hamster model showed significant reduction of the parasite load post treatment <i>via</i> the intraperitoneal route by several compounds. The preliminary pharmacokinetic evaluation of a representative compound <b>4mf</b> <i>via</i> the oral route, however, indicated high systemic clearance from the body.