901290-21-9Relevant academic research and scientific papers
Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening
Baulard, Alain R.,Biela, Alexandre,Blaise, Mickael,Bourbiaux, Kevin,Cantrelle, Francois-Xavier,Djaout, Kamel,Flipo, Marion,Frita, Rosangela,Hanoulle, Xavier,Herledan, Adrien,Kremer, Laurent,Leroux, Florence,Moune, Martin,Pintiala, Catalin,Piveteau, Catherine,Tanina, Abdalkarim,Vandeputte, Alexandre,Willand, Nicolas,Déprez, Benoit,Fa?on, Léo,Wintjens, René
, (2020)
Mycobacterium tuberculosis (M.tb), the etiologic agent of tuberculosis, remains the leading cause of death from a single infectious agent worldwide. The emergence of drug-resistant M.tb strains stresses the need for drugs acting on new targets. Mycolic acids are very long chain fatty acids playing an essential role in the architecture and permeability of the mycobacterial cell wall. Their biosynthesis involves two fatty acid synthase (FAS) systems. Among the four enzymes (MabA, HadAB/BC, InhA and KasA/B) of the FAS-II cycle, MabA (FabG1) remains the only one for which specific inhibitors have not been reported yet. The development of a new LC-MS/MS based enzymatic assay allowed the screening of a 1280 fragment-library and led to the discovery of the first small molecules that inhibit MabA activity. A fragment from the anthranilic acid series was optimized into more potent inhibitors and their binding to MabA was confirmed by 19F ligand-observed NMR experiments.
Synthesis, analgesic and anti-inflammatory evaluation of some novel quinazoline derivatives
Alafeefy, Ahmed M.,Kadi, Adnan A.,Al-Deeb, Omar A.,El-Tahir, Kamal E.H.,Al-Jaber, Nabila A.
scheme or table, p. 4947 - 4952 (2010/11/20)
Two series of some new 2,4,6-trisubstituted-quinazoline derivatives were prepared and screened for their analgesic, anti-inflammatory activity and acute toxicity. Four compounds were more potent analgesic agents than the reference drug Indomethacin and thirteen compounds showed significant anti-inflammatory activity. Seven compounds showed combined ability to inhibit both pain and inflammation. Compounds tested for acute toxicity showed no toxic symptoms or mortality rates 24 h post-administration implying their good safety margin.
