| 摘要 |
<p>1,5-diaryl-2-alkylpyrrole-3-substituted nitro esters, of Formula (I) are provided. Such compounds are potent and selective COX-2 inhibitors which are able to release NO in concentrations that make it possible to counteract the side effects due to selective COX-2 inhibition, without giving rise to hypotensive effects. Formula (I) includes compounds wherein the groups R′and R″are:—H,—F,—Cl,—Br,—CH3,—CF3,—OCH3,—SCH3, R1 is methyl, ethyl, trifluoromethyl, hydroxymethyl, methoxymethyl and the substituent in position−3 of the pyrrole ring is a chain, where the groups X, Y, Z, W and R2 are: X is a carbonyl or a group—(CHR3)—, Y is an oxygen atom or the group—NR3—and Z is a carbonyl or a group—(CHR3)—, or a [—CH(COOH)—] group, or a group—(NR3)—, W is an aliphatic chain substituted with one or two (—O—NO2) groups, R2 is:—H,—OH,—OCH3, or—NHR3. R3 is:—H,—CH3,—CH2CH3, [—CH2(CH3)2]. R′″is methylsulphonyl or sulphonamido. Pharmaceutical formulations and methods of making an using such formulations are also provided.</p> |
