Abstract

Four-Substituted derivatives of salicylic and anthranilic acids: 2-hydroxy-5-azidosulfonylbenzoic acid (HASBA, 1), 2-acetyloxy-5- azidosulfonylbenzoic acid (AASBA, 2), 2-acetamido-5- azidosulfonylbenzoic acid (AMASBA, 3) and 2-acetamido-5-sulfonamidobenzoic acid (AMSABA, 4) were synthesized and evaluated for their analgesic, antipyretic, anti-inflammatory and cytotoxic activities. HASBA, AASBA and AMASBA showed higher analgesic activity than aspirin (ASA) at 100 mg/kg dose, while AMSABA showed the least analgesic property. AMASBA exhibited higher antipyretic activity than paracetamol (PCM), while HASBA, AASBA and AMSABA also showed antipyretic effects which were of equal potency to that of PCM. The order of anti-inflammatory effects of the four compounds is: AASBA > AMASBA > HASBA > AMSABA. The effects of the substituents on the biological activities of the synthesized compounds are discussed.

Key words: Salicylic acid derivatives, anthranilic acid, analgesic, anti-inflammatory, antipyretic, cytotoxicity.