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-¿-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-1,1¿-pyrido[3,4-b]indole]-3¿-carboxylic acid (IC50 = 0.389 ± 0.015 ¿M) and 2¿-Benzoyl 2¿,3¿,4¿,9¿-tetrahydrospiro[cyclohexane-1,1¿-pyrido[3,4-b]indole]-3¿-carboxylic acid (IC50 = 00.469 ± 0.032 ¿M) compounds were to be of similar potency as that of standard drug sodium cromoglycate (IC50 =0.489 ± 0.003¿M).