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conferenceseries
.com
July 17-19, 2017 Chicago, USA
3
rd
International Conference on
Organic and Inorganic Chemistry
Volume 6, Issue 2 (Suppl)
Organic Chem Curr Res, an open access journal
ISSN:2161-0401
Organic Chemistry 2017
July 17-19, 2017
Peramivir
analogs bearing hydrophilic substituent to overcome viral resistance
Din-Chi Chiu
and
Jim-Min Fang
National Taiwan University, Taiwan
I
nfluenza an acute respiratory disease remains to impact public health greatly. One of the envelope proteins called
Neuraminidase (NA) acts as a critical role in replication cycle of influenza virus, and its inhibitors such as oseltamivir
and
peramivir
have been widely used for clinical treatment of influenza infections. Despite NA’s high conservation, certain
mutations such as H274Y and R292K have been observed, thus leading to suppression of drug effectiveness. Referring to
the co-crystal structure of NA and
peramivir
or oseltamivir, the drop of drug activity can be attributed to those unfavorable
interactions between the hydrophobic substituents, 3-pentyl or 3-pentoxyl, on NA inhibitors and amino acid residues of NA.
Consequently,
peramivir
derivatives bearing hydrophilic side chain were designed and synthesized in order to overcome drug
resistance. (Fig.1) Gratifying, a pioneering method with complete consumption of the dipolariphile was developed by using
reduced amount of nitrile oxide 1, 3-dipole to conduct the 1, 3- dipolar cycloaddition reactions. Aside from discovery of
an alternative synthetic route, alleviated drug resistance is observed on analogs with various hydrophilic substituents, and
improvement of inhibitory effects toward mutant viruses can be expected.
Biography
Din-Chi Chiu has received his BS from Department of Material Science and Engineering, National Chiao Tung University. He is motivated by the passion on organic
synthesis and drug discovery. He’s currently majoring Chemistry in National Taiwan University and conducting research about development of new anti-influenza
agent as his master study.
dylan82729@gmail.comDin-Chi Chiu et al., Organic Chem Curr Res 2017, 6:2 (Suppl)
DOI: 10.4172/2161-0401-C1-020