Anti-inflammatory and analgesic activities of some newly synthesized pyridinedicarbonitrile and benzopyranopyridine derivatives.
In continuation of our search for new substituted pyridine based anti-inflammatories, reaction of 1-(2-thienyl or furanyl)-3-(2-hydroxyphenyl)-2-propen-1-ones (1) with malononitrile in alcoholic KOH solution afforded a mixture of 4-alkoxy-2-(2-thienyl or furanyl)-5H-[1]benzopyrano[3,4-c]pyridine-5-ones (2) and 2-alkoxy-4-amino-6- (2-thienyl or furanyl)-3,5-pyridinedicarbonitriles (3). Some of the synthesized compounds were evaluated for their anti-inflammatory and analgesic activities compared to diclofenac potassium as positive control. Detailed synthesis, spectroscopic and toxicity data are reported.
Hosni
Hanaa M
HM
Pesticide Chemistry Department, National Research Centre Doki, Cairo, Egypt. hanaanrc@yahoo.com
Abdulla
Mohamed M
MM
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D001578:Benzopyrans / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D002351:Carrageenan; D004008:Diclofenac / Q000494:pharmacology; D004195:Disease Models, Animal; D005260:Female; D006358:Hot Temperature; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control*; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D015394:Molecular Structure; D009570:Nitriles / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D010146:Pain / Q000209:etiology / Q000503:physiopathology / Q000517:prevention & control*; D010147:Pain Measurement; D017288:Pain Threshold / Q000187:drug effects; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D013057:Spectrum Analysis / Q000379:methods; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D001578:Benzopyrans; D009570:Nitriles; D011725:Pyridines; D004008:Diclofenac; D002351:Carrageenan