Aminosalicylic acid antibacterial activity

Substitution of an amino group into the molecule affords an iigent with antibacterial activity. Although seldom used alone, l, ira- aminosalicylic acid (PAS, 7) has been employed as an adjunct Id streptomycin and isoniazid in treatment of tuberculosis. 

This drug possesses antibacterial activity with respect to a few cocci and colon bacillus. It exhibits a simultaneous, pronounced healing effect in patients with nonspecific ulcerative colitis, which is explained by the degradation in the body of 5-aminosalicylic acid and sulfapyridine, which possess anti-inflammatory and antibacterial properties. It is used for ulcerative colitis, chronic rhenmatoid arthritis as well as acnte and snbacnte inflammatory diseases. Synonyms of this drng are slazopyrin, salazosnlfapyridine, and others. 

Sulfasalazine is a prodrug of which 70% is converted by colon bacteria to two active metabolites, sulfapyri-dine and 5-aminosalicylic acid (mesalamine). Sulfa-pyridine has antibacterial activities, and 5-aminosali-... 

Sulfasalazine is absorbed poorly from the GI tract after oral administration 70 to 90% is transported to the colon where intestinal flora metabolize the drug to its active ingredients, sulfapyridine (antibacterial) and 5-aminosalicylic acid (antiinflammatory), which exert their effects locally. 

Since aminocoumarins have been found to exert some antibacterial activity [377], investigations were started to explore tuberculostatic activity of various coumarins related to p-aminosalicylic acid (55). 7-Amino-4-methylcoumarin (56) was found to be about one-half, and ffa s-p-aminocinnamic acid (57) one-fourth, as active as p-aminosalicylic acid [392]. The tuberculostatic action of 7-amino-4-methylcoumarin is probably dependent on the opening of the lactone... 

---