Synthesis, Biological Evaluation, and Molecular Modeling Studies of Chiral Chloroquine Analogues as Antimalarial Agents

Author:

Kondaparla Srinivasarao1,Debnath Utsab1ORCID,Soni Awakash2,Dola Vasantha Rao1,Sinha Manish1,Srivastava Kumkum2,Puri Sunil K.2,Katti Seturam B.1

Affiliation:

1. Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, India

2. Parasitology Division, CSIR-Central Drug Research Institute, Lucknow, India

Abstract

In a focused exploration, we designed, synthesized, and biologically evaluated chiral conjugated new chloroquine (CQ) analogues with substituted piperazines as antimalarial agents. In vitro as well as in vivo studies revealed that compound 7c showed potent activity ( in vitro 50% inhibitory concentration, 56.98 nM for strain 3D7 and 97.76 nM for strain K1; selectivity index in vivo [up to at a dose of 12.5 mg/kg of body weight], 3,510) as a new lead antimalarial agent.

Funder

Council of Scientific and Industrial Research

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Reference39 articles.

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