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.com
Volume 8
Medicinal Chemistry
ISSN: 2161-0444
Medicinal Chemistry 2018
June 14-15, 2018
June 14-15, 2018 | Barcelona, Spain
10
th
World Congress on
Medicinal Chemistry and Drug Design
Development of 3, 5-dinitrophenyl containing heterocycles: Structure-antimycobacterial activity
relationships studies
Galina Karabanovich
Charles University, Czech Republic
O
ur research focuses on the design and synthesis of novel nitro group containing heterocyclic compounds with high and
selective antimycobacterial efficiency and on the study of relationships between their structure and antimycobacterial
activities/toxicities. Previously described 1-alkyl-5-(3,5-dinitrobenzyl)sulfanyl-1H-tetrazoles and 2-alkyl-5-(3,5-dinitrobenzyl)
sulfanyl-1,3,4-oxadiazoles showed outstanding activities against drug-susceptible and drug-resistant strains of
Mycobacterium
tuberculosis (M. tuberculosis.).
Their minimum inhibitory concentrations reached 0.5 μm and 0.03 μm, respectively.
Moreover, 1, 3, 4-oxadiazole derivatives were active against replicating and nonreplicating strains of
z
. Described compounds
demonstrated selective effect on mycobacteria as were inactive against tested fungi and bacteria and exhibited low
in vitro
genotoxicity and toxicity in mammalian cell lines. Current work continues to study the role of individual fragments of
previously described molecules in their biological properties. We focused on influence of the heterocycle and Benzylsulfonyl
linker on antimycobacterial activity. Results of
in vitro
evaluation showed that both fragments play a significant role in the
antimycobacterial efficacy of target compounds. Moreover, alkyl/aryl substituents on heterocycle could also affect compounds
efficacy.
Biography
Galina Karabanovich has completed her PhD at the Faculty of Pharmacy in Hradec Kralove, Charles University. Currently, she occupies the Postdoctoral position at
the same University. She has published 12 papers, majority of them in medicinal chemistry journals. Her research interests are focused on the design and synthesis
of compounds with potential antimycobacterial activity; study of the relationships between structure and antimycobacterial activity of prepared substances; synthesis
of dexrazoxane analogues.
karabang@faf.cuni.czGalina Karabanovich, Med chem (Los Angeles) 2018, Volume 8
DOI: 10.4172/2161-0444-C1-039