Mon, 18 Dec 2017

Synthesis of Pyranoquinoline Derivatives and In-Silico Anti-Malarial Activity Using Docking Studies

N Pramod1*, N. C. Sree Vaishnavi1, M. Nagendra Babu1, S. Afroz Begum1, C. Gopinath1Y Pradeep Kumar1

1. Annamacharya College of Pharmacy, Department of Pharmaceutical Chemistry, Rajampet, Kadapa District, Andhra Pradesh, India.


ABSTRACT

Novel pyrano quinolone derivatives were synthesized by the treatment of p-methyl acetanilide upon treatment with DMF and POCL3 at 00 C it undergone cyclization reaction which gives 2-chloro-6-methyl quinolone-3-carbaldehyde and further treated the reaction with 4M HCL gives 2-hydroxy-6methyl quinolone-3-carbaldehyde is formed. The above reaction further treated with ethyl aceto acetate and piperidine by using grind stone technique with the elimination of ethanol and water gives 3-acetyl-7-methyl-2H- Pyrano[2,3-b] quinolone-2-one. The above reaction was further treated with 40% KOH and ethanol with different substituted aldehyde to give novel pyrano quinoline derivatives. Compounds which are synthesized are identified by MP and TLC as well as characterized by IR, 1HNMR and MASS spectroscopy. Docking studies were performed for anti-malarial activity using Plasmodium falciparum lactate dehydrogenase for a selected compounds shows good binding energy when compared to Chloroquine which is used as standard.

Keywords: Vilsmeier Hacck reagent, pyrano quinolones, docking.


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