Synthesis of the new analogs of morpholine and their antiplasmodial evaluation against the human malaria parasite Plasmodium falciparum

Author:

Upadhyay Charu1,Sharma Neha2,Kumar Sumit1,Sharma Prem Prakash2,Fontinha Diana3,Chhikara Bhupender S.4,Mukherjee Budhaditya5ORCID,Kumar Dhruv6ORCID,Prudencio Miguel3ORCID,Singh Agam P.7ORCID,Poonam 1ORCID

Affiliation:

1. Department of Chemistry, Miranda House, University of Delhi, Delhi, India

2. Laboratory for Translational Chemistry and Drug Discovery, Department of Chemistry, Hansraj College University Enclave, University of Delhi, Delhi 110007, India

3. Instituto de Medicina Molecular, Faculdade de Medicina, Universidade de Lisboa, Avenida Professor Egas Moniz, 1649-028 Lisboa, Portugal

4. Department of Chemistry, Aditi Mahavidyalaya, University of Delhi, Delhi, India

5. School of Medical Science and Technology, IIT Kharagpur, Kharagpur-721302, India

6. Amity Institute of Molecular Medicine & Stem Cell Research, Amity University Uttar Pradesh, Noida, India

7. Infectious Diseases Laboratory, National Institute of Immunology, Aruna Asaf Ali Marg, New Delhi 110067, India

Abstract

A series of morpholine analogs functionalized with hydroxyethylamine (HEA) pharmacophore was synthesized and assayed for the initial screening against Plasmodium falciparum 3D7 in culture, which suggested that analog 6k is a hit molecule with an inhibitory concentration of 5.059 ± 0.2036 μM.

Funder

Science and Engineering Research Board

Publisher

Royal Society of Chemistry (RSC)

Subject

Materials Chemistry,General Chemistry,Catalysis

Reference56 articles.

1. New leads for drug repurposing against malaria

2. Plasmodium falciparum: Multidrug resistance

3. PfEMP1: An antigen that plays a key role in the pathogenicity and immune evasion of the malaria parasite Plasmodium falciparum

4. World Health Organization: World malaria report 2020, https://www.who.int/publications/i/item/9789240015791 , accessed march 22, 2021

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