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Biological Evaluation of 2-aminothiazole Hybrid as Antimalarial and Antitrypanosomal Agents: Design and Synthesis

[ Vol. 18 , Issue. 2 ]

Author(s):

Surender S. Jadav, Vishnu N. Badavath*, Ramesh Ganesan, Narayana M. Ganta, Dominique Besson* and Venkatesan Jayaprakash*   Pages 101 - 108 ( 8 )

Abstract:


Background: A series of 2-aminothiazole schiff’s bases (1-24) were synthesized and screened against a few neglected tropical disorders (NTDs). Compounds 12 and 14 were found to have antitrypanosidal activity, whereas compound 14 was found to be more effective than standard benznidazole. The antiplasmodial assay provided three specific and effective compounds (9, 12 and 24) than standard chloroquine. Compound (21) inhibited Leishmania infantum, almost similar to Miltefosine.

Methods: All the compounds were subjected to cytotoxicity assay and none of the compounds were found to be cytotoxicity. Molecular docking simulations revealed that four compounds (1, 9, 12 and 21) were found to similarly occupy the hydrophobic active site of trans-2-enoyl acyl carrier protein reductase of P. falciparum (PfENR) as triclosan and outcomes were closely related to their anti-malarial potencies.

Results and Conclusion: The screening results against T. cruzi, T. brucei, L. donovani, L. infantum, P. falciferum and cytotoxicity assays provided a few significant to most potent compounds; two variant class of NTDs.

Keywords:

2-aminothiazole hybrid, antimalarial activity, anti-trypanosomal activity, anti-leishmanial activity, cytotoxicity studies, molecular docking simulatin.

Affiliation:

Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand, Department of Chemistry, Indian Institute of Technology, Banaras Hindu University, Varanasi, 221005, Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand, Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand, Special Programme for Research and Training in Tropical Diseases, World Health Organization, Geneva, Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand

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