Conventional and Microwave‐Assisted Synthesis of Benzimidazole Derivatives and Their In Vitro Inhibition of Human Cyclooxygenase |
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| Authors: | Daniela Secci Adriana Bolasco Melissa D'Ascenzio Flavio della Sala Matilde Yáñez Simone Carradori |
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| Institution: | 1. Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma “La Sapienza”, , 00185 Rome, Italy;2. Departamento de Farmacología and Instituto de Farmacia Industrial, Universidad de Santiago de Compostela, E‐15782 Santiago de Compostela (La Coru?a), , Spain |
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| Abstract: | A large series of 1,2‐diaryl‐benzimidazole and 2‐aryl‐1H‐benzimidazole derivatives were synthesized with slight differences using both microwave irradiation and conventional heating methods. Usually higher yields and time reactions reduction were obtained with the former method. All compounds were assayed for their in vitro ability to inhibit human cyclooxygenases, and most of them showed an encouraging inhibitory activity and isoform selectivity in the micromolar range. |
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