Antileishmanial assessment of isoxazole derivatives against L. donovani

Sushobhan Mukhopadhyay; Dinesh S. Barak; R. Karthik; Sarvesh K. Verma; Rabi S. Bhatta; Neena Goyal; Sanjay Batra

doi:10.1039/D0MD00083C

Antileishmanial assessment of isoxazole derivatives against L. donovani†

Sushobhan Mukhopadhyay,‡^a Dinesh S. Barak,‡^a R. Karthik,‡^b Sarvesh K. Verma,^c Rabi S. Bhatta,

^cd Neena Goyal*^bd and Sanjay Batra

*^ad

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* Corresponding authors

^a Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India
E-mail: batra_san@yahoo.co.uk, s_batra@cdri.res.in

^b Biochemistry Division, CSIR-Central Drug Research Institute, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India
E-mail: neena_goel@cdri.res.in

^c Pharmacokinetics Division, CSIR-Central Drug Research Institute, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India

^d Academy of Scientific and Innovative Research, CSIR- Human Resource Development Centre, (CSIR-HRDC) Campus, Sector 19, Kamla Nehru Nagar, Ghaziabad-201002, India

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 4mfvia the oral route, however, indicated high systemic clearance from the body.

This article is part of the themed collection: Neglected Tropical Diseases

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DOI: https://doi.org/10.1039/D0MD00083C
Article type: Research Article
Submitted: 09 Mar 2020
Accepted: 23 Jun 2020
First published: 20 Jul 2020

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RSC Med. Chem., 2020,11, 1053-1062

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Antileishmanial assessment of isoxazole derivatives against L. donovani

S. Mukhopadhyay, D. S. Barak, R. Karthik, S. K. Verma, R. S. Bhatta, N. Goyal and S. Batra, RSC Med. Chem., 2020, 11, 1053 DOI: 10.1039/D0MD00083C

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RSC Medicinal Chemistry

Antileishmanial assessment of isoxazole derivatives against L. donovani†

Abstract

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Antileishmanial assessment of isoxazole derivatives against L. donovani

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