2. Academic Validation
  3. Antileishmanial assessment of isoxazole derivatives against L. donovani

Antileishmanial assessment of isoxazole derivatives against L. donovani

  • RSC Med Chem. 2020 Jul 20;11(9):1053-1062. doi: 10.1039/d0md00083c.
Sushobhan Mukhopadhyay 1,  Dinesh S Barak 1,  R Karthik 2,  Sarvesh K Verma 3,  Rabi S Bhatta 3 4,  Neena Goyal 2 4,  Sanjay Batra 1 4
Affiliations

Affiliations

  • 1 Medicinal and Process Chemistry Division , CSIR-Central Drug Research Institute , Sector 10, Jankipuram Extension, Sitapur Road , Lucknow 226031 , India . Email: batra_san@yahoo.co.uk ; Email: s_batra@cdri.res.in.
  • 2 Biochemistry Division , CSIR-Central Drug Research Institute , Sector 10, Jankipuram Extension, Sitapur Road , Lucknow 226031 , India . Email: neena_goel@cdri.res.in.
  • 3 Pharmacokinetics Division , CSIR-Central Drug Research Institute , Sector 10, Jankipuram Extension, Sitapur Road , Lucknow 226031 , India.
  • 4 Academy of Scientific and Innovative Research , CSIR- Human Resource Development Centre , (CSIR-HRDC) Campus, Sector 19, Kamla Nehru Nagar , Ghaziabad-201002 , India.
PMID: 33479698 DOI: 10.1039/d0md00083c
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.

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