Synthesis of novel 1-pyrazolylpyridin-2-ones as potential anti-inflammatory and analgesic agents.

A new series of 4-alkyl/aryl-2-oxo-1-pyrazolyl-1,2-dihydropyridine-3-carbonitriles, pyrazolo[3,4-b]pyridine-5-carbonitriles and pyrido[2,3-d]pyrimidine-6-carbonitriles have been synthesized and tested for their anti-inflammatory and analgesic activities. Among the tested compounds, 3e and 8b exhibited comparable anti-inflammatory activity to the standard (indomethacin). Compounds 5, 7a, and 8b displayed potent analgesic activity.

Synthesis and antitumor activity of some novel quinazoline derivatives bearing the biologically active thione moiety.

The reactivity of isothiocyanate 1 towards some nitrogen nucleophils was investigated. Thus, interaction of 1 with p-flouroaniline, benzylamine, 2-aminopyridine, and 4-aminoantipyrine yielded the corresponding quinazoline derivatives 3-7, respectively. Triazolo-quinazoline 10 was obtained in good yield via reaction of isothiocyanate 1 with thiosemicarbazide.