ChemInform Abstract: 1,2‐Dihydro‐1‐oxopyrrolo(3,2,1‐kl)phenothiazine‐2‐carboxamides and Congeners, Dual Cyclooxygenase/5‐Lipoxygenase Inhibitors with Antiinflammatory Activity.

Abstract

1,2-Dihydro-1-oxopyrrolo(3,2,1-kl)phenothiazine-2-carboxamides and Congeners, Dual Cyclooxygenase/5-Lipoxygenase Inhibitors with Antiinflammatory Activity.-More than 50 tetracyclic lactams such as (I) are converted to the derivatives (III), e.g. (IIIa) -(IIId), as outlined in the reaction scheme and tested for antiinflammatory activity. The compound (IIIa) shows a potent cyclooxygenase/5-lipoxygenase inhibition of arachidonic acid metabolism. It is active in the rat foot edema test for antiinflammatory effect and in the mouse phenylbenzoquinone-induced writhing test for analgesic effect. (No yields given). -(MYLARI, B. L.; CARTY, T.

A new scaffold of topoisomerase I inhibitors: Design, synthesis and biological evaluation

“…The interest in topoisomerase I as a therapeutic target promoted various efforts to identify other chemotypes effective as topoisomerase inhibitors and chemical/modelling efforts to rationally design specific analogs among known inhibitors [8,9,10,11] . During the last years several tetra-and pentacyclic structures containing the indoline fragment has received much attention due to the structural correlation with natural compounds belonging to the alkaloids class endowed with biological activity as cyclooxygenase/5-lipooxygenase inhibitors, characterized by the presence of the pyrrolo[3,2-de]acridine subunit [12] , indolocarbazoles non-CPT topo I inhibitors [13,14,15,16] and analogues of physostigmine alkaloids [17,18,19,20] .…”