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Updated: Jan 27, 2026

A Colorimetric Assay of Citrate Synthase Activity in Drosophila Melanogaster
Published on: January 16, 2020
New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular
Laurent R Chiarelli1, Matteo Mori2, Giangiacomo Beretta3
1a Department of Biology and Biotechnology "L Spallanzani" , University of Pavia , Pavia , Italy.
Abstract:
Starting from the analysis of the hypothetical binding mode of our previous furan-based hit (I), we successfully achieved our objective to replace the nitro moiety, leading to the disclosure of a new lead exhibiting a strong activity against MbtI. Our best candidate 1 h displayed a Ki of 8.8 µM and its antimycobacterial activity (MIC99 = 250 µM) is conceivably related to mycobactin biosynthesis inhibition. These results support the hypothesis that 5-phenylfuran-2-carboxylic derivatives are a promising class of MbtI inhibitors.
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