Antileishmanial assessment of isoxazole derivatives againstL. donovani

A chemical library comprising substituted 3-nitroisoxazoles and 3-aminoisoxazoles was prepared and screened for their antileishmanial activity againstL. donovani. As compared to Miltefosine, the standard drug used in bioassays, several compounds displayed remarkably better inhibition of the promastigote and amastigote stages of parasites. Thein vivoevaluation of a few compounds in a golden hamster model showed significant reduction of the parasite load post treatmentviathe intraperitoneal route by several compounds. The preliminary pharmacokinetic evaluation of a representative compound4mfviathe oral route, however, indicated high systemic clearance from the body.