Antileishmanial assessment of isoxazole derivatives against L. donovani
Sushobhan Mukhopadhyay1, Dinesh S Barak1, R Karthik2
1Medicinal and Process Chemistry Division , CSIR-Central Drug Research Institute , Sector 10, Jankipuram Extension, Sitapur Road , Lucknow 226031 , India . Email: batra_san@yahoo.co.uk ;
Abstract:
A chemical library comprising substituted 3-nitroisoxazoles and 3-aminoisoxazoles was prepared and screened for their antileishmanial activity against L. 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. The in vivo evaluation of a few compounds in a golden hamster model showed significant reduction of the parasite load post treatment via the intraperitoneal route by several compounds. The preliminary pharmacokinetic evaluation of a representative compound 4mf via the oral route, however, indicated high systemic clearance from the body.
More Related Videos
08:48Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
Published on: January 26, 2016
12:02An Efficient Method for the Synthesis of Peptoids with Mixed Lysine-type/Arginine-type Monomers and Evaluation of Their Anti-leishmanial Activity
Published on: November 2, 2016
Related Concept Videos
Leishmaniasis
Anthelminthic Agents
Antiprotozoal Agents
