1. 6-Nitrobenzimidazole derivatives: Potential phosphodiesterase inhibitors: Synthesis and structure–activity relationship
- Author
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Khan, K.M., Shah, Zarbad, Ahmad, V.U., Ambreen, N., Khan, M., Taha, M., Rahim, F., Noreen, S., Perveen, S., Choudhary, M.I., and Voelter, W.
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BENZIMIDAZOLE derivatives , *PHOSPHODIESTERASE inhibitors , *CHEMICAL synthesis , *STRUCTURE-activity relationship in pharmacology , *ENZYME inhibitors , *DRUG synergism - Abstract
Abstract: 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±16.7μM. Compounds 30 (IC50 =1.5±0.043μM), 1 (IC50 =2.4±0.049μM), 11 (IC50 =5.7±0.113μM), 13 (IC50 =6.4±0.148μM), 14 (IC50 =10.5±0.51 μM), 9 (IC50 =11.49±0.08μM), 3 (IC50 =63.1±1.48μM), 10 (IC50 =120.0±4.47μM), and 6 (IC50 =153.2±5.6μM) showed excellent phosphodiesterase inhibitory activity, much superior to the standard EDTA (IC50 =274±0.007μM), 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. [Copyright &y& Elsevier]
- Published
- 2012
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