Synthesis and pharmacological evaluation of marine bromopyrrole alkaloid-based hybrids with anti-inflammatory activity

Hybrids of bromopyrrole alkaloids with aroyl hydrazone feature were synthesized and evaluated for their anti-inflammatory activity using the carrageenan induced rat paw edema method. All the tested hybrids showed good anti-inflammatory activity with 64.78-86.03% inhibition of edema. Most active hybrids 4b and 4f were further investigated for antihistaminic H-1 [4b -8.09 mu g/mL (18.5 mu M); 4f -9.26 mu g/mL (24.05 mu M)] and anti-serotonergic 5-HT3 [4b -7.01 mu g/mL (16.04 mu M); 4f -9.64 lg/ mL (25.04 mu M)] activities. Molecule 4f with anti-inflammatory, anti-histaminic and anti-serotonergic activities emerges as a potential anti-inflammatory lead form in this study. (C) 2014 King Saud University. Production and hosting by Elsevier B.V.