The effect of ten phenazine-derivatives in comparison to clofazimine on the production of prostaglandin E2 by polymorphonuclear leucocytes

Abstract

The antileprosy drug clofazimine (B663) apart from its antimycobacterial effects has been shown to stimulate the production of prostaglandin E2 (PGE2) by polymorphonuclear leucocytes (PMNL). To separate these two activites on a molecular basis a limited number of ten phenazine-derivatives was investigated for their effects on prostaglandin synthesis. It was found that the p-chlorophenyl- and p-chloroanilino-groups in position 10 and 3 of the phenazine molecule respectively were indispensable for stimulation of PGE2 production by PMNL, whereas modifications of the imino-isopropyl-group in position 2 did not affect this activity but as shown previously decreased the antimycobacterial effects of the agents against murine tuberculosis.