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Synthesis of spiro [chroman-2, 4′-piperidin]-4-one derivatives as acetyl-CoA carboxylase inhibitors

P Shinde, SK Srivastava, R Odedara, D Tuli…

文献索引:Shinde, Pundlik; Srivastava, Sanjay K.; Odedara, Rajendra; Tuli, Davinder; Munshi, Siralee; Patel, Jitendra; Zambad, Shitalkumar P.; Sonawane, Rajesh; Gupta, Ramesh C.; Chauthaiwale, Vijay; Dutt, Chaitanya Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 3 p. 949 - 953

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被引用次数: 25

摘要

Various spiro [chroman-2, 4′-piperidin]-4-one derivatives (38a–m and 43a–j) have been designed, synthesized and evaluated for in vitro acetyl-CoA carboxylase (ACC) inhibitory activity. Several compounds have shown ACC inhibitory activity in low nanomolar range. Compound 38j reduced the respiratory quotient (RQ) in C57BL/6J mice indicating increase in whole body fat oxidation even in the presence of high carbohydrate diet. Structure– ...