54294-33-6

Upstream product

• 54294-32-5 [1,3]thiazinan-2-one benzoylhydrazone; hydrobromide 
• 3414-94-6 3-phenyl-4,5-dihydro-1H-1,2,4-triazole-5-thione 
• 109-64-8 1,3-dibromo-propane 
• 613-94-5 benzoic acid hydrazide 
• 93-58-3 benzoic acid methyl ester 
• 65-85-0 benzoic acid 
• 664308-50-3 3-(3-mercapto-5-phenyl-[1,2,4]triazol-4-yl)-propan-1-ol 

Relevant academic research and scientific papers

Metal beta-lactamase inhibitor

The invention discloses application of a triazole compound, or a stereoisomer thereof, or a salt thereof, or a solvate thereof, represented by formula I in preparation of a metal beta-lactamase inhibitor drug, and belongs to the field of medicinal chemistry. The invention further discloses a preparation method of compounds, and a pharmaceutical composition comprising the compounds.

Discovery of [1,2,4]triazole derivatives as new metallo-β-lactamase inhibitors

The emergence and spread of metallo-β-lactamase (MBL)-mediated resistance to β-lactam antibacterials has already threatened the global public health. A clinically useful MBL inhibitor that can reverse β-lactam resistance has not been established yet. We here report a series of [1,2,4]triazole derivatives and analogs, which displayed inhibition to the clinically relevant subclass B1 (Verona integron-encoded MBL-2) VIM-2. 3-(4-Bromophenyl)-6,7-dihydro-5H-[1,2,4]triazolo [3,4-b][1,3]thiazine (5l) manifested the most potent inhibition with an IC50 (half-maximal inhibitory concentration) value of 38.36 μM. Investigations of 5l against other B1 MBLs and the serine β-lactamases (SBLs) revealed the selectivity to VIM-2. Molecular docking analyses suggested that 5l bound to the VIM-2 active site via the triazole involving zinc coordination and made hydrophobic interactions with the residues Phe61 and Tyr67 on the flexible L1 loop. This work provided new triazole-based MBL inhibitors and may aid efforts to develop new types of inhibitors combating MBL-mediated resistance.

Synthesis and tuberculostatic activity of 1,3-thiazacycloalkyl[3,2-b]-1,2, 4-triazoles

The 4-hydroxyalkyl-1,2,4-triazole-3-thiones cyclization allowed us to work out the effective method of 1,3-thiazacycloalkyl[3,2-b]-1,2,4-triazoles synthesis. Some of the compounds that were obtained were tested for their tuberculostatic activity. Copyrigh