23 / 30
Page 95
conferenceseries
.com
Volume 7
Pharmaceutical Regulatory Affairs: Open Access
ISSN: 2167-7689
Pharma Europe 2018
May 07-09, 2018
May 07-09, 2018 | Frankfurt, Germany
15
th
Annual European Pharma Congress
Synthesis, anti-bacterial activity and molecular docking of novel pyrazole-thiazolidinone conjugates
Ebenezer O Oluwakemi, Ashona Singh-Pilay, Neil Koorbanally
and
Parvesh Singh
University of KwaZulu-Natal, South Africa
A
novel series of pyrazole conjugates were synthesized through Vilsmeier Haack and nucleophilic substitution reaction.
The chemical structures of these compounds were established using 1HNMR, 13CNMR, IR and elemental analyses.
The synthesized compounds were assayed 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
). Interestingly, 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) were the most cogent antimicrobial compounds with minimum
bacterial concentration (MBC) of 0.08, 0.08, 0.16 and 0.16 μg/mL against MRSA and S. aureus respectively. To explore the
antimicrobial result on a structural basis, molecular docking studies of the synthesized compounds into the crystal structure
of topoisomerase II and topoisomerase IV using AutoDock Vina suggested that compounds 3a and 4b would form hydrogen
bonds with the active site of the target.
216075690@stu.ukzn.ac.zaPharmaceut Reg Affairs 2018, Volume 7
DOI: 10.4172/2167-7689-C1-031