Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Antibacterial Activity and Structure-Activity Relationship Studies of 4- aryl/alkyl-1-(diphenylacetyl)thiosemicarbazides

Author(s): Edyta Kusmierz, Agata Siwek, Urszula Kosikowska, Anna Malm, Joanna Stefanska, Katarzyna Dzitko, Monika Wujec.

Abstract:

Twenty-two 4-aryl/alkyl-1-(diphenylacetyl)thiosemicarbazides were synthesized and their in vitro antibacterial potency was evaluated. 4-(4-Chlorophenyl)-1-diphenylacetylthiosemicarbazide showed comparable activity to control antibacterial ampicillin against Gram-positive species with MICs range 3.91-15.63 µg/mL. The compound was also tested for its cytotoxicity against L929 cell line using the MTT assay technique. The results of antibacterial activity and toxicity test indicated that it display antibacterial activity at non-cytotoxic concentrations. Finally, some structural and electronic parameters have been determined in hope to get insight into different biological activity of closely related isomers.

Keywords: Antibacterial activity, Structure-activity relationship (SAR) studies, Thiosemicarbazide derivatives.

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Article Details

VOLUME: 10
ISSUE: 8
Year: 2013
Page: [748 - 757]
Pages: 10
DOI: 10.2174/15701808113100890028
Price: $58