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Crystallography 2018
Structural Chemistry & Crystallography Communication
ISSN: 2470-9905
Page 69
June 04-05, 2018
London, UK
3
rd
Edition of International Conference on
Advanced Spectroscopy,
Crystallography and Applications
in Modern Chemistry
L
eishmaniasis is caused by protozoa parasites of the genus
Leishmania, a biologically diverse group of flagellate parasites.
Leishmaniasis is endamic in tropical and subtropical regions,
particularly Afghanistan, Iran, China, Nepal, Bangladesh, etc.
Based on the high prevalence of Leishmaniasis in Pakistan and
associated morbidity, our research group has started to work on
this disease by using different strategies. Present lecture will
cover the results of structural modification of antileishmanial
natural product and a commercially available drug by using a
crystal engineering approach co-crystallization. Co-crystals
are crystalline structures made up of two or more components
in a definite stoichiometric ratio linked through non-covalent
interactions in same crystal lattice. They differ in their biological
and physiochemical properties from their components. They
have wide applications in drug designing and in analysis of
active pharmaceutical ingredients (APIs). The co-crystals of
anti-leishmainal natural product, sesselin (1) and an anti-cancer
drug exemestane (2) with thiourea were synthesized by using
neat grinding followed by liquid assisted grinding and solution
methods. Both the pure sesseline, exemestane and their co-
crystalized form with thiourea, (1 and 2, respectively) were
evaluated for their anti-leishmanial activity in vitro against L.
major promastegoates. The co-crystal (1) exhibited improved
leishmanicidal activity (IC50 = 13.2 + 1.2 ug/mL) in comparison
to that of sesseline (IC50 = 29.4 + 1.0 ug/mL). However, the co-
crystal of exemestane with thiourea (2) found to be in active.
dr.sammer.yousuf@gmail.comCO-CRYSTALLIZATION- TOWARDS ENHANCED BIOLOGICAL ACTIVITIES
EXAMPLES OF CRYSTAL ENGINEERING APPROACH
Sammer Yousuf
and
M. Iqbal Choudhary
University of Karachi, Pakistan
Struct Chem Crystallogr Commun 2018, Volume 4
DOI: 10.21767/2470-9905-C1-006