合成螺[色满-2,4'-哌啶]-4-酮衍生物作为乙酰辅酶 A 羧化酶抑制剂。
Synthesis of spiro[chroman-2,4'-piperidin]-4-one derivatives as acetyl-CoA carboxylase inhibitors.
机构信息
Medicinal Chemistry, Torrent Research Centre, Torrent Pharmaceuticals Ltd, PO Bhat, Gandhinagar 382428, Gujarat, India.
出版信息
Bioorg Med Chem Lett. 2009 Feb 1;19(3):949-53. doi: 10.1016/j.bmcl.2008.11.099. Epub 2008 Dec 3.
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-activity relationship (SAR) has been discussed.
各种螺[色满-2,4'-哌啶]-4-酮衍生物（38a-m 和 43a-j）已被设计、合成并评估其体外乙酰辅酶 A 羧化酶（ACC）抑制活性。一些化合物在纳摩尔范围内表现出 ACC 抑制活性。化合物 38j 降低了 C57BL/6J 小鼠的呼吸商（RQ），表明即使在高碳水化合物饮食存在的情况下，全身脂肪氧化也增加。讨论了构效关系（SAR）。
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