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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
Synthesis, anti-bacterial activity and molecular docking of novel pyrazole conjugates
Ebenezer O Oluwakemi, Neil Koorbanally
and
Parvesh Singh
University of KwaZulu-Natal, South Africa
A
novel series of pyrazole conjugates were synthesized using molecular hybridization approach through Vilsmeier-Haack
reaction. The structure elucidation of the synthesized compounds was established using 1HNMR, 13CNMR, IR and
elemental analyses. All compounds were tested for antimicrobial activity against two Gram positive bacteria (Methicillin-
resistant
Staphylococcus aureus, Staphylococcus aureus)
and four Gram negative bacteria
(Escherichia coli, Salmonella
typhimurium, Klebsiella pneumonia
and
Pseudomonas aeruginosa)
. Among the compounds tested, 3-(2,4-dichlorophenyl)-1-
(2,4-dinitrophenyl)-1pyrazoyl)methylene)hydrazinecarbothioamide (3a) and 2-((3-(2-chlorophenyl)-1-(2,4-dinitrophenyl)-
1H-pyrazol-4-yl)methyleneamino)thiazolidin-4-one (4b) emerged as themost cogent antimicrobial compoundswithminimum
bacterial concentration (MBC) of 0.08, 0.08, 0.16 and 0.16 μg/mL against MRSA and
S. aureus
respectively. Molecular docking
studies of the compounds into the crystal structure of topoisomerase II and topoisomerase IV suggested that compounds 3a
and 4b preferably interact with the target through hydrogen bonding.
216075690@stu.ukzn.ac.zaMed chem (Los Angeles) 2018, Volume 8
DOI: 10.4172/2161-0444-C1-040