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2-Amino/Azido/Hydrazino-5-alkoxy-5H-[1]benzopyrano[4,3-d]pyrimidines:Synthesis and Pharmacological Evaluation

[ Vol. 3 , Issue. 2 ]

Author(s):

O. Bruno, C. Brullo, F. Bondavalli, A. Ranise, S. Schenone, M. Tognolini, V. Ballabeni and E. Barocelli   Pages 127 - 134 ( 8 )

Abstract:


New series of 5-alkoxy-benzopyranopyrimidine derivatives were developed from the chemical modulation of the substituent in position 2 of the scaffold, with the aim to produce analgesic/antiphlogistic agents more potent than analogues previously reported. The 2-hydrazino derivatives exhibited a good analgesic activity in writhing test; the analgesic doses of the compounds did not affect mice spontaneous locomotor activity thus any confounding sedative effect could be excluded. These derivatives revealed an aspirin-like profile with a strong inhibition of AA-induced platelet aggregation, probably due to a strong, non selective, inhibition of cyclooxygenases. In spite of the inhibition of COX activity displayed in vitro, the compounds did not cause gastric damage in rats after acute oral administration. A different pharmacological profile was observed for the 2-azido derivatives, particularly in vivo.

Keywords:

2-Amino/Azido/Hydrazino-5-alkoxy-5H-[1]benzopyrano[4,3-d]pyrimidines, analgesic activity, antinociceptive activity, antiphlogistic activity, antiplatelet activity, COX1/COX2 inhibition

Affiliation:

Viale Benedetto XV, 3-16132 Genova, Italy.



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