40357-87-7

Usage

Uses

Used in Pharmaceutical Industry:
4-Hydroxy-1-Methyl-1h-pyridin-2-one is used as a reactant for the synthesis of 3-deaza-3-halouracil nucleosides, which exhibit cytostatic activity in three cancer cell lines. These nucleosides have the potential to be developed into effective anti-cancer drugs, making 4-Hydroxy-1-Methyl-1h-pyridin-2-one a valuable starting material in the development of novel cancer treatments.

Upstream product

• 53937-03-4 N‐methyl‐4‐benzyloxy‐2‐pyridone 
• 626-03-9 3-deazauracil 
• 77-78-1 dimethyl sulfate 
• 53937-02-3 4‐benzyloxy‐2‐hydroxy‐pyridine 
• 53937-02-3 4-(benzyloxy)pyridin-2(1H)-one 

Downstream Products

• 41759-19-7 4-methoxy-1-methyl-2-pyridone 
• 1613057-54-7 3-(4-butylphenyl)-4-hydroxy-1-methylpyridin-2(1H)-one 
• 1613057-55-8 3-(3,5-dimethylphenyl)-4-hydroxy-1-methylpyridin-2(1H)-one 
• 1613057-57-0 3-(biphenyl-4-yl)-4-hydroxy-1-methylpyridin-2(1H)-one 
• 1613057-58-1 4-hydroxy-1-methyl-3-o-tolyl-pyridin-2(1H)-one 
• 92-52-4 biphenyl 
• 1613057-52-5 4-hydroxy-1-methyl-3-phenylpyridin-2(1H)-one 
• 1613057-53-6 C₁₂H₁₂N₂O₄ 

Relevant academic research and scientific papers

Umpolung-like Cross-coupling of Tosylhydrazones with 4-Hydroxy-2-pyridones under Palladium Catalysis

Tosylhydrazones under palladium catalysis were found to perform cross-coupling reactions with 4-hydroxy-2-pyridones. The umpolung-like reactivity, between the α-carbon of tosylhydrazone and the 3-position of the heterocycle, which is observed in the obtai

TRICYCLIC GYRASE INHIBITORS FOR USE AS ANTIBACTERIAL AGENTS

Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

Synthesis and biological evaluation of 3,3-difluoropyridine-2,4(1H,3H)- dione and 3-deaza-3-fluorouracil base and nucleoside derivatives

New 3-deaza-3-halouracil nucleosides including 3-deaza-3-fluorouridine and its 2′-deoxy and arabino analogues have been prepared by fluorination of protected precursors. The resulting 3,3-difluoropyridine-2,4(1H,3H)-dione derivatives underwent palladium-c

Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: Intelligent design and evolution through the judicious use of structure-guided design and stucture-activity relationships

The discovery of new antibacterial agents with novel mechanisms of action is necessary to overcome the problem of bacterial resistance that affects all currently used classes of antibiotics. Bacterial DNA gyrase and topoisomerase IV are well-characterized clinically validated targets of the fluoroquinolone antibiotics which exert their antibacterial activity through inhibition of the catalytic subunits. Inhibition of these targets through interaction with their ATP sites has been less clinically successful. The discovery and characterization of a new class of low molecular weight, synthetic inhibitors of gyrase and topoisomerase IV that bind to the ATP sites are presented. The benzimidazole ureas are dual targeting inhibitors of both enzymes and possess potent antibacterial activity against a wide spectrum of relevant pathogens responsible for hospital- and community-acquired infections. The discovery and optimization of this novel class of antibacterials by the use of structure-guided design, modeling, and structure-activity relationships are described. Data are presented for enzyme inhibition, antibacterial activity, and in vivo efficacy by oral and intravenous administration in two rodent infection models.

Novel sulfonate analogues of combretastatin A-4: Potent antimitotic agents

Sulfonate analogues of combretastatin A-4 have been prepared. These compounds compete with colchicine and combretastatin A-4 for the colchicine binding site on tubulin and are potent inhibitors of tubulin polymerization and cell proliferation. Importantly, these compounds also inhibit the proliferation of P-glycoprotein positive (+) cancer cells, which are resistant to many other antitumor agents.

Benzopyrans

A compound of the formula: STR1 or a pharmaceutically acceptable salt thereof, wherein X is O, S or NH; R and R1 are each independently selected from H and C1 -C4 alkyl or taken together represent C2 -C6 alkylene; R2 is H or C1 -C4 alkyl; R3 is a 6-membered heterocyclic ring containing 2N hetero-atoms, said ring being linked to X by a ring carbon atom, optionally benzo-fused and optionally substituted, including in the benzo-fused portion, by C1 -C6 alkyl, hydroxy, --OR5, halo, --S(O)m R5, oxo, amino, --NHR5, --N(R5)2, cyano, --CO2 R5, --CONH2, --CONHR5 or --CON(R5)2, with the proviso that R3 is not an N--(C1 -C6 alkyl)pyridonyl group; R4 is phenyl substituted by a hydroxy group and optionally further substituted by 1 or 2 substitutents each independently selected from hydroxy, C1 -C6 alkyl, --OR5, halo, cyano and nitro; R5 is C1 -C6 alkyl; R6 is --OR5, --NHR5, --N(R5)2, --SR5 or --NHR9 ; R7 is cyano; R8 is --OR5, --NHR5, --N(R5)2, or --NHR9 ; R9 is phenyl optionally substituted by C1 -C6 alkyl, hydroxy, --OR5, halo, cyano or nitro; and m is 0, 1 or 2.