ISSN:
1420-908X
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Abstract It was found that a number of substitute 2-phenyl-1,3-indandiones possesses a considerable inhibitory effect on the classical pathway of complement. Furthermore it appeared that in this series a reasonable correlation (r=0.86) exists between this anti-complement effect and the inhibition of the prostaglandine biosynthesis. A quantitative structure-activity relation study revealed that both the electronic σ parameter of the substituent involved and the lipophilicity of the corresponding compound are important for anti-complement activity. Mainly the C5 step in the complement process is inhibited by these compounds. The complement-inhibiting phenylindandiones also inhibit the alternative pathway. This effect may also be due to an inhibition of C5, as C5 is common to both pathways. Remarkably, the 2-(3,5-dichlorophenyl)-1,3-indandione, which is most active in the anti-complement test, showed no reduction of the carrageenan-induced oedema in the rat after both oral and local application. Possibly the absence of this anti-inflammatory effect is caused by the pharmacokinetic profile of the compound.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01972374
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