Synthesis of 12β-methyl-18-<i>nor</i>-avicholic acid analogues as potential TGR5 agonists-Reference-Cited by-同舟云学术

Synthesis of 12β-methyl-18-nor-avicholic acid analogues as potential TGR5 agonists

Published:2022 Issue:17 Volume:20 Page:3511-3527
ISSN:1477-0520
Container-title:Organic & Biomolecular Chemistry
language:en
Short-container-title:Org. Biomol. Chem.

Author:

Ure Elizabeth M.¹,Harris Lawrence D.¹^ORCID,Cameron Scott A.¹^ORCID,Weymouth-Wilson Alex²,Furneaux Richard H.¹^ORCID,Pitman Janet L.³^ORCID,Hinkley Simon. F.¹^ORCID,Luxenburger Andreas¹^ORCID

Affiliation:

1. Ferrier Research Institute, Victoria University of Wellington, 69 Gracefield Rd, Lower Hutt 5040, New Zealand

2. ICE Group, 68 Weld Street, RD2, Palmerston North 4472, New Zealand

3. School of Biological Sciences, Victoria University of Wellington, Kelburn Parade, Wellington 6012, New Zealand

Abstract

A series of 12β-methyl-18-nor-avicholic acid analogues was prepared and evaluated for activity at TGR5 and FXR. Compounds 46 and 53 emerged as low-micromolar TGR5 agonists, providing potential new templates for further development.

Funder

Ministry of Business, Innovation and Employment

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2022/OB/D1OB02401A

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