Antiinflammatory, analgesic and kinase inhibition activities of some acridine derivatives

Abstract

9-Chloro-2,4-(un)substituted acridines (1) on condensation with sulpha-diazine, sulphathiazole, and sulphaacetamide gave condensation products 3a-h. 3-Aryl-4-phenyl-2-imino-4-thiazolines (4) on condensation with 9-chloro-2,4-(un)substituted acridines (1) gave condensation products 5a-5o. Both 3a-3h and 5a-5o were puri ed by crystallization or by chromatography. Structures assigned to 3a-3h and 5a-5o are supported by correct spectral data. Antiin®ammatory and analgesic activity screening of 3a, 3e, 3f and 5a-5c, 5e, 5g, 5i, 5m, 5n were carried out using carrageenin induced paw oedema and phenyl quinone writhing assay. Some of the compounds exhibited interesting antiin®ammatory or analgesic activities.

Synthesis, crystal structure of some new 2‐(4‐methylbenzoylimino)‐3‐aryl‐4‐methyl‐1,3‐thiazolines

“…2-Phenylimino-1,3-thiazoline-4-acetanilides have shown significant antifungal activity against rice blast Pyricularia oryzae, thus can be used as agrochemical fungicides [15]. The condensation products of 3-aryl-4-phenyl-2-imino-4-thiazolines with 9-chloro-2,4-(un)substituted acridines exhibited interesting antiinflammatory and analgesic activities [16]. Atropisomerism has been observed in some N,N-diaryl-2-iminothiazoline derivatives.…”

Microbial activity of some heterocyclic Schiff bases and metal complexes: A review

“…These include bacteria [29,30], fungi [31], and viruses [32,33], which are discussed subsequently in this review. Moreover, benzimidazole Schiff bases have also been reported to have antioxidant, anti-inflammatory, analgesic, antitumor, anticancer, and inhibitory properties [34][35][36][37][38][39].…”

Effect of Substituents on the Regioselectivity of the Reaction of α‐Tosyloxyketones with Thioureas in Acidic Medium: Access to 2‐Aminothiazoles and 2‐Imino‐2,3‐dihydrothiazoles

“…The use of 2‐imino‐2,3‐dihydrothiazoles II as precursors to synthesize a wide variety of compounds also makes them compounds of interest , so an efficient and simple method is needed to synthesize 2‐imino‐2,3‐dihydrothiazoles by which we can vary substituents present at various positions.…”