Monoterpene Citral Derivatives as Potential Antimalarials

Author:

Singh Soni1,Khandare Reena P.1,Sharma Manish2,Bhasin Virendra K.2,Bhat Sujata V.1

Affiliation:

1. Advanced Research Laboratory in Natural and Synthetic Chemistry, V. G. Vaze College, Mumbai University, Mithagar Road, Mulund (E), Mumbai 4000 081, India

2. Molecular Parasitology Laboratory, Department of Zoology, University of Delhi, Delhi 110007, India

Abstract

Conjugated acid derivatives containing nitrogen have been synthesized from the simple acyclic monoterpene citral, using various reactions, including Wittig, Baylis Hillman, amide and ester condensations. Similarly, amine peroxides were synthesized by subjecting citral to Mannich type reaction with amines and t-butyl hydroperoxide. Molecules 3–10 were evaluated for antimalarial activity against erythrocytic stages of chloroquine sensitive P. falciparum strain 3D7. Four derivatives displayed interesting activity with an IC50< 2.5 μM, and warrant further investigations.

Publisher

SAGE Publications

Subject

Complementary and alternative medicine,Plant Science,Drug Discovery,Pharmacology,General Medicine

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