220731-02-2

Upstream product

• 2942-59-8 2-chloronicotinic acid 
• 1071-46-1 hydrogen ethyl malonate 
• 1315320-58-1 C₉H₆ClN₃O 
• 49609-84-9 2-Chloronicotinoyl chloride 

Downstream Products

• 701977-68-6 Ethyl 3-(3-Bromoanilino)-2-(2-Chloronicotinoyl) Acrylate 
• 477251-77-7 ethyl 1-(3-bromophenyl)-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxylate 
• 500355-37-3 N-isopropyl-1-[(3-phenylethynyl)phenyl]-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide 
• 500355-51-1 N-isopropyl-1-[3-(3-hydroxy-3-phenylbut-1-ynyl)phenyl]-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide 
• 477251-78-8 1-(3-Bromophenyl)-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxylic Acid 
• 477251-79-9 N-Isopropyl-1-(3-bromophenyl)-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide 
• 220729-07-7 ethyl 1,4-dihydro-4-oxo-1-phenyl-1,8-naphthyridine-3-carboxylate 
• 1391033-55-8 C₁₇H₁₄N₂O₃ 
• 1391033-56-9 ethyl 1-benzyl-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylate 
• 1391033-57-0 ethyl 1,4-dihydro-1-(4-methoxybenzyl)-4-oxo-1,8-naphthyridine-3-carboxylate 
• 1391033-58-1 ethyl 1-(4-chlorobenzyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylate 
• 1391033-59-2 ethyl 1,4-dihydro-4-oxo-1-(4-trifluoromethylbenzyl)-1,8-naphthyridine-3-carboxylate 
• 220729-13-5 ethyl 1,4-dihydro-1-(4-methoxyphenyl)-4-oxo-1,8-naphthyridine-3-carboxylate 
• 220729-16-8 ethyl 1-(4-chlorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylate 

Relevant academic research and scientific papers

Substituted pyrido[2,3-c]pyridazin-4(1H)-ones as tumor necrosis factor alpha and phosphodiesterase 4 inhibitors

The present invention pertains to field of medical technology, specifically relates to a pyridino-oxopyridazine derivative of formula (I), its pharmaceutically acceptable salts, its stereoisomers or its solvates, wherein R1, R2, Rsu

Ethyl 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylates by a tandem S NAr-addition-elimination reaction

A series of N-substituted 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylate esters has been prepared in two steps from ethyl 2-(2-chloronicotinoyl)acetate. Treatment of the β-ketoester with N,N-dimethylformamide dimethyl acetal in N,N-dimethylformamide (DMF) gave a 95% yield of the 2-dimethylaminomethylene derivative. Subsequent reaction of this β-enaminone with primary amines in DMF at 120oC for 24 h then afforded the target compounds in 47-82% yields by a tandem SNAr-addition-elimination reaction. Synthetic and procedural details as well as a mechanistic rationale are presented.

1,8-Naphthyridine-3-carboxamide derivatives with anticancer and anti-inflammatory activity

A number of 1-propargyl-1,8-naphthyridine-3-carboxamide derivatives (15-35) have been synthesized and screened for their in vitro cytotoxicity and anti-inflammatory activity. Compounds 22, 31 and 34 have shown high cytotoxicity against a number of cancer cell lines, while compound 24 showed significant anti-inflammatory activity.

Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: Identification of MK-0873, a potent and effective PDE4 inhibitor

A SAR study of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides is described. Optimization of the series was based on in vitro potency against PDE4, inhibition of the LPS-induced production of TNF-α in human whole blood and minimizing affinity f

Anticancer and anti-inflammatory activities of 1,8-naphthyridine-3-carboxamide derivatives

Several 1,8-naphthyridine-3-carboxamide derivatives (8-23) were synthesized and tested for in vitro cytotoxicity against eight cancer cell lines and a normal cell line. Compound 12 exhibited high cytotoxicity (IC50 = 1.37 μM) in HBL-100 (breast) cell line while compounds 17 (IC50 = 3.7 μM) and 22 (IC50 = 3.0 μM) have shown high cytotoxicity in KB (oral) and SW-620 (colon) cell lines, respectively. The synthesized 1,8-naphthyridine-3-carboxamides were also evaluated for anti-inflammatory and myeloprotective activities, indicated by modulation in cytokine and chemokine levels secreted by dendritic cells.