69466-91-7Relevant academic research and scientific papers
Synthesis of 3-(3-aryl-pyrrolidin-1-yl)-5-aryl-1,2,4-triazines that have antibacterial activity and also inhibit inorganic pyrophosphatase
Lv, Wei,Banerjee, Biplab,Molland, Katrina L.,Seleem, Mohamed N.,Ghafoor, Adil,Hamed, Maha I.,Wan, Baojie,Franzblau, Scott G.,Mesecar, Andrew D.,Cushman, Mark
, p. 406 - 418 (2014/01/17)
Inorganic pyrophosphatases are potential targets for the development of novel antibacterial agents. A pyrophosphatase-coupled high-throughput screening assay intended to detect o-succinyl benzoic acid coenzyme A (OSB CoA) synthetase inhibitors led to the unexpected discovery of a new series of novel inorganic pyrophosphatase inhibitors. Lead optimization studies resulted in a series of 3-(3-aryl-pyrrolidin-1-yl)-5-aryl-1,2,4-triazine derivatives that were prepared by an efficient synthetic pathway. One of the tetracyclic triazine analogues 22h displayed promising antibiotic activity against a wide variety of drug-resistant Staphylococcus aureus strains, as well as activity versus Mycobacterium tuberculosis and Bacillus anthracis, at a concentration that was not cytotoxic to mammalian cells.
New heteroaromatic aminations on 5-aryl-1,2,4-triazines and 1,2,4,5-tetrazines by palladium catalysis
Pellegatti, Laurent,Vedrenne, Emeline,Leger, Jean-Michel,Jarry, Christian,Routier, Sylvain
experimental part, p. 4383 - 4389 (2010/07/05)
The efficient and original palladium-catalyzed amination of 5-Aryl-1,2,4-triazines and 1,2,4,5-tetrazines is reported. This Buchwald-Hartwig type reaction leads to the formation of aminated heterocycles via methylsulfur release. The reaction is optimized and a wide range of amines is used to determine the scope and limitations of this methodology.
Pharmacologically active substituted 1,2,4-triazines
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, (2008/06/13)
Substituted 1,2,4-triazines, compositions thereof and methods of using same are described. The compounds of the invention exhibit a wide range of pharmacological activity including anti-inflammatory, analgesic, anti-pyretic, hypotensive and central nervous system effects.
