Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry and Computational Chemistry

Abstract

Design, synthesis, docking and evolution of fused imidazoles as antiinflammatory and antibacterial agents

Author(s): Galal A. M. Nawwar, Nabil M. Grant, Randa H. Swellem and Samia A. M. Elseginy

New benzimidazole and imidzopyridine derivatives were designed and synthesized from their corresponding oximes II. The newly synthesized compounds were investigated in vivo for their anti-inflammatory and analgesic activities. Some of the new compounds (IVc, IVf, IVi) showed reasonable anti-inflammatory and analgesic activity in experimental rats in comparing to indomethacin and Diclofenac Na, as reference drugs Moreover, some of the newly synthesized compounds tested as antimicrobial agents, IVh exhibited potent antimicrobial activities with low MIC in comparing with Cefoperazone and Fluconazole as reference drugs Docking studies was carried out for derivatives of highest anti-inflammatory activity into the COX-2 binding site. Designed compounds IVc,IVf,IVi revealed a similar binding mode to COX-2 inhibitor.


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