3-(1,3,4-Thiadiazole-2-yl)quinoline derivatives: synthesis, characterization and anti-microbial activity.

Abstract

A new series of thiadiazoles and intermediate thiosemicarbazones were synthesized from the chloroquinone molecule, with an aim to explore their effect on in vitro growth of microorganisms causing microbial infection. The chemical structures of the compound were elucidated by elemental analysis, FTIR, 1H and 13C NMR and ESI-MS spectral data. In vitro anti-microbial activity was performed against Staphylococcusaureus, Streptococcuspyogenes, Salmonellatyphimurium, and Escherichiacoli. The MIC was detected using the double dilution method. The results were compared by calculating percent inhibit area/μg of the compounds and the standard "amoxicillin". The selected compounds were tested for cytotoxic results using MTT assay H9c2 cardiac myoblasts cell line and the results showed that all the compounds offered remarkable >80% viability to a concentration of 200 μg/mL.

• Authors: Abdul R Bhat, Tazeem, Amir Azam, Inho Choi, Fareeda Athar
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 46 Issue 7 Pg. 3158-66 (Jul 2011) ISSN: 1768-3254 [Electronic] France
• PMID: 21530014 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2011 Elsevier Masson SAS. All rights reserved.

Chemical References

• Anti-Bacterial Agents
• Hydroxyquinolines
• Thiadiazoles
• Thiosemicarbazones

Topics

• Animals
• Anti-Bacterial Agents (chemical synthesis, pharmacology)
• Cell Line
• Cell Survival (drug effects)
• Escherichia coli (drug effects, growth & development)
• Hydroxyquinolines (chemical synthesis, pharmacology)
• Microbial Sensitivity Tests
• Myocytes, Cardiac (cytology, drug effects)
• Rats
• Salmonella typhimurium (drug effects, growth & development)
• Staphylococcus aureus (drug effects, growth & development)
• Streptococcus pyogenes (drug effects, growth & development)
• Thiadiazoles (chemical synthesis, pharmacology)
• Thiosemicarbazones (chemical synthesis, pharmacology)