SYNTHESIS AND BIOLOGICAL EVALUATION OF MAST CELL STABILIZERS

The role of mast cells can be protective or harmful: depending upon the physiological/pathological condition in which they get activated. The latter role is due to mast cell degranulation and the release of an array of incendiary mediators. Mast cells have a well-established role in diseases like allergy eczema anaphylactic shock mastocytosis and other miscellaneous mast cell disorders. The derivatives of spiro-β-carboline were evaluated for mast cell stabilization activity by compound 48/80 induced degranulation histamine release assay. The mast cell stabilization of 2′-Heptyl-2′3′4′9′-tetrahydrospiro[cyclohexane-11′-pyrido[34-b]indole]-3′-carboxylic acid (IC50 = 0.389 ± 0.015 μM) and 2′-Benzoyl 2′3′4′9′-tetrahydrospiro[cyclohexane-11′-pyrido[34-b]indole]-3′-carboxylic acid (IC50 = 00.469 ± 0.032 μM) compounds were to be of similar potency as that of standard drug sodium cromoglycate (IC50 =0.489 ± 0.003μM).