Studies on benzhydryl derivaties. I. Synthesis and anti-inflammatory activity.

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A series of N-diphenylmethyl derivatives of glycine was synthesized and their anti-inflammatory and some other pharmacological properties were studied. The inhibition of carrageenin edema-induction and the protection of albumin from heat denaturation by these derivatives were studied in relation to the substituents in one of the phenyl groups. The most potent compounds, 3, 4-dichloro-(Compd. 22) and 4-fluoro-(Compd. 16) diphenylmethylglycine derivatives, showed the higher activity in carrageenin-edema and weaker toxicity tested by gastric irritation and acute toxicity study than 2-(4-isobutyl-phenyl) propionic acid (ibuprofen). Compd. 16 showed the significant and interesting synergic effect by co-administration with cortisone acetate in the various tests of anti-inflammatory activity.

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