Lead optimization studies towards the discovery of novel carbamates as potent AChE inhibitors for the potential treatment of Alzheimer's disease

KK Roy, S Tota, T Tripathi, S Chander, C Nath…

文献索引：Roy, Kuldeep K.; Tota, Santoshkumar; Tripathi, Tusha; Chander, Subhash; Nath, Chandishwar; Saxena, Anil K. Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 21 p. 6313 - 6320

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被引用次数: 9

摘要

The optimization of our previous lead compound 1 (AChE IC50= 3.31 μM) through synthesis and pharmacology of a series of novel carbamates is reported. The synthesized compounds were evaluated against mouse brain AChE enzyme using the colorimetric method described by Ellman et al. The three compounds 6a (IC50= 2.57 μM), 6b (IC50= 0.70 μM) and 6i (IC50= 2.56 μM) exhibited potent in vitro AChE inhibitory activities comparable to the drug ...