The College of Pharmacy discussed the MSc thesis entitled “Design, Synthesis and Preliminary Pharmacological Evaluation of New Quinolone-Antioxidant Conjugates” by the student Shahad Rafid Abdul Alkhalik and the supervisor, Associate Professor Tagreed N-A Omar, at the Pharmaceutical Chemistry Deportment. The study aimed to synthesize new derivatives of antioxidants and quinolones via acetate linkage with high efficacy as anti-inflammatory and antimicrobial activity and study the absorption, distribution, metabolism, and excretion properties of the final compounds. The study included using Schrodinger software for virtual design and analysis of quinolone derivatives and antioxidants and evaluation of biological activities such as antimicrobial activity against Gram-positive and Gram-negative bacteria and Candida albicans in vitro and in vivo as anti-inflammatory activity in reducing the thickness of paw edema in rats. The ester group was introduced at the C3 position of quinolones with antioxidants via an acetate linkage, a step that is rarely addressed as most previous studies have focused on the linkage via the NH group. The study concluded that the compounds were successfully synthesized and the bioactivity results were obtained, and the results of their bioactivity study indicated that the final compounds have drug-like properties.The study recommended studying the toxic activity of the synthesized derivatives as well as the anti-cancer activity and the initial hydrolysis in diluted plasma and at pH levels (1.2 and 7.4) and their affinity for lipids.
