Synthesis, spectral characterizations and molecular docking studies of Montelukast Methyl Ketone, Lacosamide derivatives as promising antibacterial agents and antiviral activity towards New Castle Disease Virus (NDV) using Embryonated Chicken Eggs Assay (ECEA)
Year: 2026
Type: article
Abstract: In the present study, we report the synthesis of montelukast methyl ketone, lacosamide derivatives.The scalable procedure for the generation of montelukast (Singulair, drug for asthma) based on a novel and useful way of performing the key substitution reaction has been presented.The present approach is recognized from the prior solutions in the application of inexpensive and accessible materials, which ensures very simple and economic production method.Our suggested approach for the production of montelukast is capable to minimize an amount of impurities and lets the efficient production of montelukast and its scale-up.We retrospectively studied the efficacy and tolerability of lacosamide (LCM) in children with drug resistant epilepsy in a tertiary care centre in the Netherlands, from 2013 till 2019, with a follow-up of two years.79 children, aged < 18 years, were included.Retention rate, effectiveness, reason for termination and side-effects were analyzed.Furthermore, prognostic variables for discontinuation as well as the incidence of side-effects were determined.The LCM retention rate and effectiveness of response were analyzed at three, twelve and twenty-four months.Lacosamide (LCM) is a new generation antiepileptic drug that affects the slow inactivation of voltage-gated sodium channels.We studied whether chronic LCM treatment prior to onset of absence seizures was able to prevent/reduce the development of absence seizures in GAERS rats, a well-validated animal model of absence epilepsy and epilepto genesis.Newcastle disease is highly infectious viral disease causing huge economic losses worldwide.These losses can be prevented by control of viral diseases.Medicinal plants have been traditionally used for treatment of different diseases since long.In this study the effect of from montelukast methyl ketone are investigated against Newcastle disease virus (NDV) by an in-vivo assay.Seven groups of nine-day-old embryo nated chicken eggs were inoculated with various treatments of different concentration.All the groups except uninoculated negative control group were inoculated with velogenic NDV strain; five groups received different concentrations.Daily observe the rate of embryo survival.Allantoic fluid from treated eggs was collected for hemagglutination test.Results showed that embryo survival rate was higher 300μg/ml treated antiviral activity.The synthesized heterocyclic compounds were evaluated for their in vitro antibacterial activity against pathogenic strains of both gram negative and gram positive bacteria.The 3a derivative displayed superior antibacterial activity against E. coli, Pseudomonas aeruginosa in comparison to the reference drug.The molecular docking studies indicate that the montelukast methyl ketone (3a), lacosamide derivative (3b) binds to the cell wall protein of P. aeruginosa and E. coli by formation of amino acid residues (GLU342, LEU398) of the bacterial cell wall protein.The 3b derivatives were antiviral activity towards New Castle Disease Virus (NDV).All the products were thoroughly characterized by 1 H-NMR, 13 C-NMR, FT-IR, Mass spectral and CHN analysis.All the products were found to have good oral bioavailability.
Authors: S. Bakyalakshmi, N. Elumalai, CT. Ravichandran
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: bronze
OpenAlex ID: W7202397346