期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 33, 期 1, 页码 1444-1452出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2018.1512596
关键词
Scaffold hopping; fragments; O-acetylserine sulphhydrylase; medicinal chemistry; pyrazoles; ligand-based drug design
资金
- MSCA-ITN-2014-ETN project INTEGRATE [642620]
Several bacteria rely on the reductive sulphur assimilation pathway, absent in mammals, to synthesise cysteine. Reduction of virulence and decrease in antibiotic resistance have already been associated with mutations on the genes that codify cysteine biosynthetic enzymes. Therefore, inhibition of cysteine biosynthesis has emerged as a promising strategy to find new potential agents for the treatment of bacterial infection. Following our previous efforts to explore OASS inhibition and to expand and diversify our library, a scaffold hopping approach was carried out, with the aim of identifying a novel fragment for further development. This novel chemical tool, endowed with favourable pharmacological characteristics, was successfully developed, and a preliminary Structure-Activity Relationship investigation was carried out.
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