- One-pot synthesis of benzimidazoles in water in the presence of SiO 2-OPO3H
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Silica-bound phosphoric acid (SiO2-OPO3H), as an eco-friendly, reusable, and heterogeneous catalyst, was applied for synthesis of 2-substituted benzimidazoles in water at 70°C. Very short reaction times, clean work-up, and high yields are among the advantages of this protocol.
- Mirjalili,Bamoniri,Rahimi Kazerouni
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- 6-Nitrobenzimidazole derivatives: Potential phosphodiesterase inhibitors: Synthesis and structure-activity relationship
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6-Nitrobenzimidazole derivatives (1-30) synthesized and their phosphodiesterase inhibitory activities determined. Out of thirty tested compounds, ten showed a varying degrees of phosphodiesterase inhibition with IC50 values between 1.5 ± 0.043 and 294.0 ± 16.7 μM. Compounds 30 (IC50 = 1.5 ± 0.043 μM), 1 (IC50 = 2.4 ± 0.049 μM), 11 (IC50 = 5.7 ± 0.113 μM), 13 (IC50 = 6.4 ± 0.148 μM), 14 (IC50 = 10.5 ± 0.51 μM), 9 (IC50 = 11.49 ± 0.08 μM), 3 (IC50 = 63.1 ± 1.48 μM), 10 (IC50 = 120.0 ± 4.47 μM), and 6 (IC50 = 153.2 ± 5.6 μM) showed excellent phosphodiesterase inhibitory activity, much superior to the standard EDTA (IC50 = 274 ± 0.007 μM), and thus are potential molecules for the development of a new class of phosphodiesterase inhibitors. A structure-activity relationship is evaluated. All compounds are characterized by spectroscopic parameters.
- Khan,Shah, Zarbad,Ahmad,Ambreen,Khan,Taha,Rahim,Noreen,Perveen,Choudhary,Voelter
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experimental part
p. 1521 - 1526
(2012/04/23)
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