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Coumarin-Pyrazoline Derivatives: Their One-Pot Microwave Assisted Synthesis and Antimalarial Activity

M. Mumtaz Alam* , M. Shaquiquzzaman* , W. Akhtar* , M. Faraz Khan* , G. Verma* , M. Akhter* , A. Marella** , S. Parmar* , R Khatoon* , M. Mumtaz Alam*

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Journal of Pharmaceutical and Medicinal Chemistry 3(1):p 5-9, January - June 2017. | DOI: DOI: http://dx.doi.org/10.21088/jpmc.2395.6615.3117.1

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Abstract

The current work described the microwave assisted synthesis of various pyrazoline derivatives (3a-3i). Equimolar quantities of different chalcones and substituted hydrazine (Acetyl hydrazine or Phenyl hydrazine) were irradiated under microwave conditions to give the title compounds. These compounds were evaluated for in vitro antimalarial potential using schizont maturation inhibition assay using chloroquine sensitive 3D7 strain of P. falciparum. Amongst, all the compounds, the one with trimethoxy substitution (3g) was found to be most active with IC50 value of 11.63 g/mL. From the results, one could infer that bulky groups favoured antimalarial activity. The derivatives were also studied for antimicrobial effect against bacteria (Staphylococcus aureus and Escherichia coli) and fungi (Rhizopus oryza and Penicillum citrum).

Keywords: Pyrazoline; Microwave; Antimalarial; Antimicrobial.

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DOI: DOI: http://dx.doi.org/10.21088/jpmc.2395.6615.3117.1

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