RESEARCH ON HETEROCYCLIC-COMPOUNDS .32. SYNTHESIS AND CYCLOOXYGENASE-INDEPENDENT ANTIINFLAMMATORY AND ANALGESIC ACTIVITY OF IMIDAZO[1,2-A]PYRIMIDINE DERIVATIVES

Citation
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
Citations number
24
Categorie Soggetti
Chemistry Medicinal
ISSN journal
02235234
Volume
29
Issue
4
Year of publication
1994
Pages
279 - 286
Database
ISI
SICI code
0223-5234(1994)29:4<279:ROH.SA>2.0.ZU;2-6
Abstract
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.