72784-20-4

Upstream product

• 72786-71-1 (E)-2-Cyano-3-[5-(4-methoxy-phenylsulfanyl)-2-nitro-phenyl]-acrylamide 
• 55149-72-9 α-cyano-β-(2-nitro-5-chlorophenyl)acrylamide 
• 6628-86-0 5-chloro-2-nitrobenzaldehyde 
• 72786-73-3 2-Amino-6-(4-methoxy-phenylsulfanyl)-quinoline-3-carboxylic acid amide 
• 95-92-1 oxalic acid diethyl ester 
• 19488-09-6 sodium 4-methoxyphenylthiolate 

Relevant academic research and scientific papers

Structure-Activity Relationships in a Series of Novel 3,4-Dihydro-4-oxopyrimidoquinoline-2-carboxylic Acid Antiallergy Agents

A series of more than 50 new 3,4-dihydro-4-oxopyrimidoquinoline-2-carboxylic acid derivatives and related compounds with substituent variations at the 2, 3, and 5-9 positions was prepared and evaluated for antiallergy activity using the rat PCA assay.These compounds were obtained by the condensation of the appropriately substituted 2-aminoquinoline-3-carboxamides with dialkyl oxalates, followed by further chemical transformations.More than two-thirds of the compounds prepared exhibited intravenous activity ranging from 1 to 400 times disodium cromoglycate (DSCG).Structure-activity data suggest that the presence of a carboxylic acid moiety at the 2 position affords optimal potency and that esters are preferred for good oral absorption.Best oral activity, with ED50 values ranging from 0.3 to 3.0 mg/kg, was displayed by ethyl esters with methoxy and/or ethoxy groups at the 7 and 8 positions.