On December 1, 2016, Gampe, Christian M.; Kahne, Daniel Evan; Kahne, Suzanne Walker; Qiao, Yuan; East, Stephen; Parkes, Alastair L.; Southey, Michelle; Hunter, James; Whittaker, Mark; Arthuis, Martin published a patent.Application of 5455-98-1 The title of the patent was Preparation of 6H,7H-pyrazolo[1,5-a][1,3,5]triazin-7-one derivatives as inhibitors of bacterial glycosyl transferases. And the patent contained the following:
The title compounds of formula I [A = independently each (un)substituted C2-6 alkyl, aryl, carbocyclyl, 5-membered heteroaryl, or 6-membered heteroaryl; B = independently H or each (un)substituted alkyl, alkenyl, alkynyl, aryl, carbocyclyl, heterocyclyl, or heteroaryl; Y = a bond or each (un)substituted C1-6-alkylene, C3-6 carbocyclylene, or heterocyclylene; X = a bond, O, CH2, NRNX, NRNX-C(O)-NRNX, or (un)substituted heterocyclylene; L = a bond, O, C(O), NRLBC(O), C(O)NRLB, NRLB, or SO2; each RLB = independently H or each (un)substituted alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, or heteroaryl, or RLB and B are taken together with their intervening atoms to form an (un)substituted heterocyclic ring; R1 = H, halogen, or (un)substituted substituted C1-6 alkyl; RN1 = H, (un)substituted C1-6 alkyl, or a nitrogen protecting group; RNX = H, (un)substituted C1-6 alkyl, or a nitrogen protecting group], pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof are prepared The invention also provides pharmaceutical compositions of the compounds I for human and veterinary use. The compounds I are useful for inhibiting bacterial growth and therefore are useful in treating and/or preventing bacterial infections. Thus, 100 mg 2-(4-tert-butylphenyl)-4-(methylsulfanyl)-6H,7H-pyrazolo[1,5-a][1,3,5]triazin-7-one and 190 mg N-(3-aminopropyl)-4-chloro-3-methylaniline were dissolved in 4 mL 1,4-dioxane, heated to 130° in a microwave for 11 h, then concentrated, and purified using HPLC to give 7.9 mg 2-(4-tert-butylphenyl)-4-[[3-[(4-chloro-3-methylphenyl)amino]propyl]amino]-6H,7H-pyrazolo[1,5-a][1,3,5]triazin-7-one (II) (5% yield). II showed min. inhibitory concentration of 3.1, 2, and 4 μg/mL against methicillin-susceptible Staphylococcus aureus Newman, S. aureus 29213, and S. aureus 43300 at 24 h, resp. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Application of 5455-98-1
The Article related to bacterial infection prevention treatment pyrazolotriazinone preparation, pyrazolotriazinone preparation inhibitor bacterial glycosyl transferase antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 5455-98-1
Referemce:
Amide – Wikipedia,
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