88570-08-5Relevant academic research and scientific papers
Synthesis and antiulcer activity of (E)-5-[2-(3-pyridyl)ethenyl]-1H,7H-pyrazolo [1,5-a]pyrimidine-7-ones.
Doria,Passarotti,Sala,Magrini,Sberze,Tibolla,Ceserani,Castello
, p. 417 - 429 (2007/10/02)
A series of (E)-5-[2-(3-pyridyl)ethenyl]-1H,7H-pyrazolo-[1,5-a]pyrimidine-7-ones were synthesized and evaluated for the inhibition of stress-induced gastric ulcers in the rat after oral administration. Several molecules were found to be very active. The particularly interesting compound (E)-1-(3-chlorophenyl)-5-[2-(3-pyridyl)ethenyl]-1H,7H-pyrazolo[1,5-a]- pyrimidine-7-one was chosen for wider pharmacological investigation.
Substituted ethenyl derivatives of 1H-pyrazolo-[1,5-a]pyrimidine having gastroenteric activity, compositions thereof, and methods of using the same
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, (2008/06/13)
Compounds of the formula (I) STR1 wherein R1 is: (a) hydrogen, or C1 -C6 alkyl; (b) an unsubstituted 2-pyridyl or 3-pyridyl group; (c) a benzyl group, wherein the phenyl ring is unsubstituted or substituted by halogen, C1 -C6 alkoxy or C1 -C6 alkyl; (d) a phenyl ring, unsubstituted or substituted by one or two groups chosen from halogen, trihalomethyl, C1 -C6 alkoxy, C1 -C6 alkyl, C2 -C6 alkanoylamino, nitro and amino; each of R2 and R3 independently represents hydrogen, halogen or C1 -C6 alkyl; R4 represents a 2-pyridyl, 3-pyridyl or 4-pyridyl group, unsubstituted or substituted by C1 -C6 alkyl; and the pharmaceutically acceptable salts thereof are disclosed. The compounds have activity in the gastroenteric system, particularly anti-ulcerogenic and gastric anti-secretory activity. Additionally, the compounds have activity in reducing the undesired gastrointestinal side-effects resulting from systemic administration of anti-inflammatory prostaglandin synthetase inhibitors.
