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.
Letters in Drug Design & Discovery
Title:Antibacterial Activity and Structure-Activity Relationship Studies of 4- aryl/alkyl-1-(diphenylacetyl)thiosemicarbazides
Volume: 10 Issue: 8
Author(s): Edyta Kusmierz, Agata Siwek, Urszula Kosikowska, Anna Malm, Joanna Stefanska, Katarzyna Dzitko and Monika Wujec
Affiliation:
Keywords: Antibacterial activity, Structure-activity relationship (SAR) studies, Thiosemicarbazide derivatives.
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.
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Kusmierz Edyta, Siwek Agata, Kosikowska Urszula, Malm Anna, Stefanska Joanna, Dzitko Katarzyna and Wujec Monika, Antibacterial Activity and Structure-Activity Relationship Studies of 4- aryl/alkyl-1-(diphenylacetyl)thiosemicarbazides, Letters in Drug Design & Discovery 2013; 10 (8) . https://dx.doi.org/10.2174/15701808113100890028
DOI https://dx.doi.org/10.2174/15701808113100890028 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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