- Research on heterocyclic compounds. XXXII. Synthesis and cyclooxygenase-independent antiinflammatory and analgesic activity of imidazopyrimidine derivatives
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The synthesis of a group of imidazopyrimidine-2-carboxylic esters, acids and amides is described.The structures of the new compounds are supported by 1H- and 13C-NMR spectra.These compounds were tested in vivo for their antiinflammatory and analgesic activities as well as for their ulcerogenic action.The ester 5b, the acid 6c and the amide 7a showed antiinflammatory action in the rat paw edema (ca. 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 (ca 1/5 x indomethacin).All new compounds were found to be lacking in inhibitory activity on cyclooxygenase in vitro. imidazopyrimidines / antiinflammatory activity / analgesic activity / ulcerogenic activity / cyclooxygenase inhibition
- Abignente, E.,Sacchi, A.,Laneri, S.,Rossi, F.,D'Amico, M.,et al.
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p. 279 - 286
(2007/10/02)
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- Process for producing sulfonylureas
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There is described a novel process for producing sulfonylureas of formula I STR1 wherein R1 is hydrogen or alkyl, R2 is STR2 E is =N-- or =CH--, R3 is alkyl, alkoxy or halogen, R4 is alkyl, cycloalkyl, alkoxy, halogen, alkoxy-alkyl, halo-alkyl or halo-alkoxy, R5 is hydrogen or alkyl, T is a substituted phenyl group STR3 Y is hydrogen or halogen, X is hydrogen, halogen, alkyl, halo-alkyl, alkenyl, halo-alkenyl, alkynyl, alkoxy, halo-alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halo-alkylthio, alkylsulfonyloxy, phenylsulfonyloxy, phenylsulfonyloxy mono- or polysubstituted by alkyl, or is di-alkylsulfamoyl, and A is a bridge member which has 3 or 4 atoms and which contains 1 or 2 hetero atoms, selected from the group consisting of oxygen, sulfur and nitrogen, the said process comprising reacting a silfonamide of the formula II in the presence of a base, with diphenyl carbonate to form a salt of a phenyl carbamate converting this salt into the free phenyl carbamate and reacting this further with an amine. Sulfonylureas are herbicidally effective compounds.
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