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Organic Chemistry 2018 Journal of Organic & Inorganic Chemistry
ISSN: 2472-1123 Page 51
August 16-17, 2018
Dublin, Ireland
6th Edition of International
Conference and Exhibition on
Organic Chemistry
T he global threat of pathogenic resistance to available
therapeutic agents has become a menace to clinical practice,
public health and man’s existence in consequential. This has
therefore led to an exigency in the development of newmolecular
scaffolds with profound activity profiles. In this vein, a versatile
synthetic tool for accessing new molecules by incorporating two
or more pharmacophores into a single entity with the unique
ability to be recognized by multiple receptors hence leading to
an improved bioactivity, known as molecular hybridization, has
been explored with tremendous success. Accordingly, aware of
the similarity in pharmacological activity spectrum of quinoline
and 1,2,3-triazole pharmacophores such as; anti-Alzheimer,
anticancer, anti-HIV, antimalarial and antimicrobial to mention but
a few, the present study sets out to synthesize novel hybrids of
quinoline and 1,2,3-triazole. The new hybrids were accessed via
click chemistry using copper catalysed azide-alkyne 1,3-dipolar
cycloaddition reaction. All synthesized compounds were
evaluated for their pharmaco-potential in an antimicrobial assay
out of which the 3-OH derivative emerged as the most active with
MIC value of 4 μg/mL against Creptococcus neoformans; a value
superior tostandardFluconazoleandcomparable toAmphotericin
B. Structures of synthesized hybrids were elucidated using
appropriate spectroscopic techniques (1H, 13C and 2D NMR, FT-
IR and HRMS).
Paul Awolade
Ghana Co-Operative Credit Unions Association (CUA) Ltd, Ghana
J Org Inorg Chem 2018, Volume 4
DOI: 10.21767/2472-1123-C4-012
Synthesis of novel quinoline hybrids via molecular
hybridization and their pharmaco-potential evaluation