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

被引：34

作者：

Shinde, Pundlik ^{[1
]}

Srivastava, Sanjay K. ^{[1
]}

Odedara, Rajendra ^{[1
]}

Tuli, Davinder ^{[1
]}

Munshi, Siralee ^{[2
]}

Patel, Jitendra ^{[2
]}

Zambad, Shitalkumar P. ^{[3
]}

Sonawane, Rajesh ^{[5
]}

Gupta, Ramesh C. ^{[1
]}

Chauthaiwale, Vijay ^{[4
]}

Dutt, Chaitanya

机构：

[1] Torrent Pharmaceut Ltd, Torrent Res Ctr, Med Chem, Gandhinagar 382428, Gujarat, India

[2] Torrent Pharmaceut Ltd, Torrent Res Ctr, Cellular & Mol Biol, Gandhinagar 382428, Gujarat, India

[3] Torrent Pharmaceut Ltd, Torrent Res Ctr, Pharmacol, Gandhinagar 382428, Gujarat, India

[4] Torrent Pharmaceut Ltd, Torrent Res Ctr, Discovery Res, Gandhinagar 382428, Gujarat, India

[5] Torrent Pharmaceut Ltd, Torrent Res Ctr, Analyt Dev, Gandhinagar 382428, Gujarat, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 03期

关键词：

Acetyl-CoA carboxylase inhibitors; Spirochromanones; FATTY-ACID OXIDATION; POTENT;

D O I：

10.1016/j.bmcl.2008.11.099

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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-activity relationship (SAR) has been discussed. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：949 / 953

页数：5

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