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Volume 4, Issue 2 American Journal of Ethnomedicine
ISSN 2348-9502
Natural Products Congress & World Pharma Congress 2017
October 16-18, 2017
Page 39
Notes:
3rd World Congress on
NATURAL PRODUCTS CHEMISTRY AND RESEARCH
&
12th WORLD PHARMA CONGRESS
October 16-18, 2017 Budapest, Hungary
Peyman Salehi, American Journal of Ethnomedicine, 4:2
DOI: 10.21767/2348-9502-C1-001
Synthesis of novel norsufentanil analogues via a four-component Ugi reaction and in vivo, docking,
and QSAR studies of their analgesic activity
Novel pseudopeptide tetherednorsufentanil derivativeswere synthesizedby the four-componentUgi reaction. Norsufentanil
was reacted with succinic anhydride to produce the corresponding carboxylic acid. The resulting carboxylic acid has
undergone a multicomponent reaction with different aldehydes, amines, and isocyanides to produce a library of the desired
compounds (Scheme 1). In all cases, amide bond rotation was observed in the NMR spectra. In vivo analgesic activity of
the synthesized compounds was evaluated by a tail flick test. Very encouraging results were obtained for a number of the
synthesized products. Some of the synthesized compounds such as 5a, 5b, 5h, 5j and 5r were found to be more potent than
sufentanil, sufentanil citrate, and norsufentanil. Binding modes between the compounds and mu and delta opioid receptors
were studied by molecular docking method. The relationship between the molecular structural features and the analgesic
activity was investigated by a Quantitative Structure-Activity Relationship (QSAR) model. The results of the molecular
modeling studies and the in vivo analgesic activity suggested that the majority of the synthesized compounds were more potent
than sufentanil and norsufentanil.
Biography
Peyman Salehi received his BSc in Chemistry in 1987 from Ferdowsi University, Mashhad, Iran. Then he moved to Shiraz University where he received his MSc in 1990
and PhD in 1995 in Organic Chemistry. He started his academic work at Razi University, Kermanshah as an Assistant Professor in 1995. After five years, he moved to
Shahid Beheshti University as anAssociate Professor. Since 2005, he works as a Professor in the Department of Phytochemistry. He has published more than 160 papers
in peer reviewed international journals.
Peyman Salehi
Shahid Beheshti University, Iran