107755-79-3

Upstream product

• 34107-46-5 6-methyl-3-pyridinemethanol 
• 21684-59-3 ethyl 6-methylnicotinate 
• 53014-84-9 2-methyl-5-formylpyridine 
• 101620-10-4 4-(4-diphenyl-methyl-1-piperazinyl)butylamine 
• 118420-23-8 3-(6-Methyl-3-pyridyl)propionic acid 
• 117830-17-8 3-(6-methyl-pyridin-3-yl)-acrylic acid 

Relevant academic research and scientific papers

Acrylamide derivatives as antiallergic agents. 2. Synthesis and structure-activity relationships of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamides

A new series of 3-(3-pyridyl)acrylamides 16, 17, 19, and 26, and 5-(3-pyridyl)-2,4-pentadienamides 20-25 were prepared and evaluated for their antiallergic activity. Several of these compounds exhibited more potent inhibitory activities than the parent compounds 1a [(E)-N-[4 [4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamide] against the rat passive cutaneous anaphylaxis (PCA) reaction and the enzyme 5-lipoxygenase. Particularly, 4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3-pyridyl)acrylamide (17p) showed an ED50 value of 3.3 mg/kg po in the rat PCA test, which was one-fifth of ketotifen and oxatomide. As compared with ketotifen and oxatomide, compound 17p (AL-3264) possessed a better balance of antiallergic properties due to inhibition of chemical mediator release, inhibition of 5-lipoxygenase, and antagonism of histamine.

ω-(3-pyridyl)alkenamide derivatives and anti-allergenic pharmaceutical compositions containing same

Compounds of the formula: STR1 wherein X is alkylene or --(CR6 =CR7)r -- wherein R6 is H, alkyl or phenyl, R7 is H, alkyl, cyano or phenyl, and r is 1 or 2; A is alkylene or alkylene interrupted by at least one double bond; R1 is H, halogen, alkyl, alkoxy, alkylthio, cycloalkyloxy, cycloalkylthio, alkoxycarbonyl, carboxy, phenyl, phenoxy, phenylthio, 3-pyridyloxy or 3-pyridylthio; R2 is H, hydroxy, alkanoyloxy or alkoxycarbonyloxy, or adjacent R1 and R2 may combine to form tetramethylene or --CH2 OCR8 R9 O-- (R8 and R9 are alkyl); R3 is H, alkyl or hydroxyalkyl; R4 is H or alkyl; R5 is phenyl, heteroaryl or --(CH2)m --CHR10 R11 (R10 is H or phenyl, R11 is phenyl or pyridyl and m is 0 to 2); p is 0 or 1; and q is 2 or 3; the phenyl group or moiety being optionally substituted, and a salt thereof, process for the preparation thereof, and pharmaceutical composition containing the same. Said compounds and salts thereof show excellent antiallergic activity mainly through 5-lipoxygenase inhibiting activity, antihistamine activity and/or inhibitory activity against chemical mediator release and useful for treatment of allergic diseases.