Bioorg Med Chem Lett. 2009 Feb 1;19(3):949-53. Epub 2008 Dec 3.

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

Shinde P, Srivastava SK, Odedara R, Tuli D, Munshi S, Patel J, Zambad SP, Sonawane R, Gupta RC, Chauthaiwale V, Dutt C.

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Medicinal Chemistry, Torrent Research Centre, Torrent Pharmaceuticals Ltd, PO Bhat, Gandhinagar 382428, Gujarat, India.

Abstract

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.

PMID:: 19097787; [PubMed - indexed for MEDLINE]

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