Design and synthesis of low molecular weight compounds with complement inhibition activity

An attempt was made to synthesize a series of non-cytotoxic low molecular weight compounds of varying substitutions and functionalities having pharmacophore activity like carbonyl compounds, carboxylic acid and bioisosteres like tetrazole and phenyl acrylic acid. The in vitro assay of these analogues for the inhibition of complement activity revealed significant inhibitory activity for varying substituents and, particularly, for bioisosteres, that is, tetrazole and phenyl acrylic acid derivatives.

A series of non-cytotoxic low molecular weight aromatic tetrazoles and phenyl acrylic acid derivatives were synthesized. The in vitro assay revealed significant inhibitory activity of these compounds with IC50 values as low as 23 μM with absence of or poor intrinsic lytic properties compared to positive controls.Figure optionsDownload as PowerPoint slide