RESEARCH ON HETEROCYCLIC-COMPOUNDS .32. SYNTHESIS AND CYCLOOXYGENASE-INDEPENDENT ANTIINFLAMMATORY AND ANALGESIC ACTIVITY OF IMIDAZO[1,2-A]PYRIMIDINE DERIVATIVES
E. Abignente et al., RESEARCH ON HETEROCYCLIC-COMPOUNDS .32. SYNTHESIS AND CYCLOOXYGENASE-INDEPENDENT ANTIINFLAMMATORY AND ANALGESIC ACTIVITY OF IMIDAZO[1,2-A]PYRIMIDINE DERIVATIVES, European journal of medicinal chemistry, 29(4), 1994, pp. 279-286
The synthesis of a group of imidazo[1,2-a]pyrimidine-2-carboxylic este
rs, acids and amides is described. The structures of the new compounds
are supported by H-1- and C-13-NMR spectra. These compounds were test
ed in vivo for their antiinflammatory and analgesic activities as well
as for their ulcerogenic action. The ester 5b, the acid 6c and the am
ide 7a showed antiinflammatory action in the rat paw edema (similar to
1/3 x indomethacin), while almost all compounds displayed significant
analgesic activity in the acetic acid writhing test, particularly the
5-chloro-7 methyl derivatives 5a, 6a and 7a (similar to 1/5 x indomet
hacin). All new compounds were found to be lacking in inhibitory activ
ity on cyclooxygenase in vitro.