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Medchem & Toxicology 2018

Page 84

Journal of Organic & Inorganic Chemistry

ISSN: 2472-1123

A n n u a l C o n g r e s s o n

Medicinal Chemistry,

Pharmacology and toxicology

J u l y 3 0 - 3 1 , 2 0 1 8

Am s t e r d a m , N e t h e r l a n d s

C

onjugated nitroalkenes are valuable precursors in organic synthesis they have significant affinity to nucleophilic reagents

as diazocompounds, nitrones, ylides, carbodienes, vinyl ethers etc., additionally; nitro group may be easily converted to

many other functional groups. Subsequently it was known, that nitro group conjugated with sp

2

carbon atom stimulate many

forms of biological activity. Considering these facts we decided to check a series of (E)-2-aryl-1-cyano-1-nitroethenes as

potential antibacterial and antifungal agents but without genotoxic properties. A homogenous series of β-EWG functionalyzed

β-nitrostyrenes were synthesized and characterized by IR, UV,

1

H-NMR and

13

C-NMR spectra. Obtained compounds were screened

in vitro

against a panel of reference strains of bacteria and fungi and their cytotoxicity towards cultured human HepG2 and HaCaT

cells was established. Antimicrobial results indicated that four of synthesized compounds exhibited significant antimicrobial

activity against all tested reference bacteria and fungi belonging to yeasts with a specific and strong activity towards

B. subtilis

ATCC 6633. The details of our studies, which describe the synthesis, activity, and proposition for the mechanism of an action of

studied compounds, will be presented

.

Oleh.Demchuk@UMCS.Lublin.pl

New aspects of synthesis and microbiological

applications of

β

-EWG functionalized

β

-nitrostyrene

Oleg M Demchuk

1

, Anna Boguszewska-Czubara

2

, Karolina Kula

3

,

Artur Wnorowski

2

, Anna Biernasiuk

2

, Łukasz Popiołek

2

, Dawid

Miodowski

3

and Radomir Jasinski

3

1

Maria Curie-Skłodowska University, Lublin, Poland

2

Medical University of Lublin, Lublin, Poland

3

Cracow University of Technology, Cracow, Poland

J Org Inorg Chem 2018, Volume 4

DOI: 10.21767/2472-1123-C3-009

Figure.

Synthesis of 4-AN and 4-AN-Ac