stroke-cns-2018-posters-abstracts

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I n t e r n a t i o n a l C o n f e r e n c e o n

Neurological Disorders,

Stroke and CNS

October 22-23 , 2018

Athens , Greece

Journal of Neurology and Neuroscience

ISSN: 2171-6625

Stroke and CNS 2018

Background:

Treatment of dyslipidemia impacts directly on the cardiovascular health. The use of statin, a 3-hydroxy-3-

methylglutaryl coenzyme, a reductase inhibitor for the treatment of dyslipidemia has been associated with dose limiting

hepatoxicity, myototoxicity and tolerability due to myalgias thereby necessitating the synthesis of new drug candidates for the

treatment of lipid disorder.

Methods:

The reaction of appropriate benzenesulphonamide with substituted phenoxazinone in the presence of phenylboronic

acid gave the targeted compounds. The molecular docking study were carried out using autodock tool against peroxisome

proliferator activated receptor alpha. The

in vivo

lipid profiles were assayed using conventional methods. The kidney and liver

function test were carried out to assess the effect of the derivatives on the organs. The LD50 of the most active derivatives were

determined using mice.

Results:

The targeted compounds were successfully synthesized in excellent yields and characterized using spectroscopic

techniques. The results of the molecular docking experiment showed that they were good stimulant of peroxisome proliferator

activated receptor alpha. Compound 9f showed activity at K

of 2.8 nM and 12.6 kcal/mol of binding energy. All the compounds

tested reduced triglyceride, total cholesterol, low density lipoprotein cholesterol and very low density lipoprotein cholesterol level

in the mice model. Some of the reported compounds also increased high density lipoprotein cholesterol level in the mice. The

compounds did not have appreciable effect on the kidney and liver of the mice used. The LD

showed that the novel compounds

have improved toxicity profile.

Conclusion:

The synthesis of 15 new derivatives of carboxamides bearing phenoxazinone and sulphonamide were successful. The

compounds possessed comparable activity to gemfibrozil. The reported compounds had better toxicity profile than gemfibrozil

and could serve as a replacement for the statins and fibrate class of lipid agents.

Novel phenoxazinones as potent agonist of PPAR-

design, synthesis, molecular docking and in vivo

studies

Okafor Sunday N, Ugwu David I and Okoro Uchechukwu C

University of Nigeria, Nigeria

J Neurol Neurosci 2018, Volume: 9

DOI: 10.21767/2171-6625-C3-015