Abstract
A series of N-(acridin-9-yl)-4-(benzo[ d]imidazol/oxazol-2-yl) benzamides has been synthesized by the condensation of 9-aminoacridine derivatives with benzimidazole or benzoxazole derivatives. Condensation of 2-hydroxy naphthaldehyde with functionalized diamines leads to the formation of Schiff’s bases and not imidazole derivatives. All these compounds were characterized by correct FT-IR, 1H NMR, MS and elemental analyses. These compounds were screened for anti-inflammatory, analgesic and kinase (CDK-1, CDK-5 and GSK-3) inhibition activities. Compounds 11 and 7e( f) showed good anti-inflammatory (35.8% at 50 mg/kg po) activity and good analgesic activity (60% at 50 mg/kg po), respectively. Compound 3b showed significant in vitro activity against CDK-5 (IC 50 = 4.6 μM) and CDK-1(IC 50 = 7.4 μM) and compound 3a showed moderate CDK-5 inhibitory activity (IC 50 = 7.5 μM). The other compounds showed moderate anti-inflammatory and analgesic activities.
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