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Der Pharmacia Sinica
ISSN: 0976-8688
Eurosc i con Conference on
Medicinal Chemistry
and Biosimilars
M a r c h 2 5 - 2 6 , 2 0 1 9
B u d a p e s t , H u n g a r y
Medicinal Chemistry & Biosimilars 2019
The non-steroidal anti-inflammatory drugs (NSAIDs) are medications
widely used to relieve pain, reduce inflammation, and bring down a high
temperature. NSAIDs are used to relieve symptoms of headaches, painful
periods, sprains and strains, colds and flu, arthritis, and other causes of long-
term pain. We have used five members of the NSAIDs family as ketoprofen,
naproxen, fenoprofen, flurbiprofen and carprofen to obtain a series of new
compounds interesting for analysing their biological activity. Because of
the number of contraindications and the incompatibility of the most of the
NSAIDs with other drugs, it is of interest of obtaining new organic compounds
enclosing a profen residue in the structure of its molecule. Tryptamine is
a bicyclic heterocycle and is the most important and best characterized
member of the indole amine family. The tryptamine scaffold is regarded as
a privileged structure, due to its broad applications for designing medicinal
agents. The tryptamine and its analogues have been reported to display varied
pharmacological activities, such as antimigraine, antibacterial, antitumor etc.
In considering the significant biological activities of tryptamine and also of
the NSAIDs, it is interesting the obtaining of new compounds structurally
containing a tryptamine moiety as well as aryl propionic (NSAIDs) residue
attached thereto. In searching of easy and eco-friendly method for obtaining
of the target compounds we have found described in the literature method. The
method uses amines and carboxylic acids for obtaining amide bonds using DCC
as dehydrating agent. N, N-dicyclohexylcarbodiimide (DCC) is a dehydrating
agent commonly used for the synthesis of esters, amides or anhydrides.
DCC reacts with the carboxyl group of aryl propionic derivative to produce an
activated acylation agent that reacts with the amino group of the tryptamine
molecule to form an amide bond. The resulting five new compounds (Reaxys)
are characterized by their melting points, IR, 1H- and 13C-NMR spectra.
Biography
Iliyan Ivanov has completed MSc (1990), PhD (2003) University
of Plovdiv, Bulgaria. His research interests include synthetic
application of α-amidoalkilation reaction and development of
new methods for obtaining of N-heterocyclic compounds. He
has developed a new alternative method for the synthesis of
isoquinoline analogues. Subsequently, the method has been
successfully applied for the synthesis of novel beta-carboline,
quinazolinone, isochroman and other N- and O- heterocyclic
derivatives. He is the Author of more than 60 publications in the
field of synthesis of heterocyclic compounds.
Stanimir Manolov has received his BSc of Computer chemistry
(2008), MSc (2009) and PhD of Organic chemistry (2015)
degrees from University of Plovdiv (Bulgaria). He works as an
Assistant Professor of Organic chemistry from Mar’ 2012. In
Feb’ 2016, he was appointed as a Chief Assistant Professor of
Organic Chemistry at University of Plovdiv “Paisii Hilendarski”.
His research in the group of Prof Iliyan Ivanov is focused on the
development of new synthetic methodologies of biologically
active N and O containing natural compounds.
Synthesis of NSAIDs derivatives of tryptamine
Stanimir P Manolov, Iliyan I Ivanov, Dimitar G Bojilov and Valery
A Mollov
University of Plovdiv "Paisii Hilendarski", Bulgaria
Stanimir P Manolov et al.,Der Pharmacia Sinica 2019, Volume:10
DOI: 10.21767/0976-8688-C1-003