Recent Advances in the Medicinal Chemistry of Farnesoid X Receptor

Author(s):  
Yuanying Fang ◽  
Lamees Hegazy ◽  
Brian N. Finck ◽  
Bahaa Elgendy
Author(s):  
Antonino N. Fallica ◽  
Valeria Pittalà ◽  
Maria N. Modica ◽  
Loredana Salerno ◽  
Giuseppe Romeo ◽  
...  

Author(s):  
Joao Carlos Silva de Souza ◽  
Suzana Gomes Claudino ◽  
Rodolfo da Silva Simoes ◽  
Patricia Rufino Oliveira ◽  
Kathia Maria Honorio

F1000Research ◽  
2017 ◽  
Vol 6 ◽  
pp. 2029 ◽  
Author(s):  
John YL Chiang

Bile acids are derived from cholesterol to facilitate intestinal nutrient absorption and biliary secretion of cholesterol. Recent studies have identified bile acids as signaling molecules that activate nuclear farnesoid X receptor (FXR) and membrane G protein-coupled bile acid receptor-1 (Gpbar-1, also known as TGR5) to maintain metabolic homeostasis and protect liver and other tissues and cells from bile acid toxicity. Bile acid homeostasis is regulated by a complex mechanism of feedback and feedforward regulation that is not completely understood. This review will cover recent advances in bile acid signaling and emerging concepts about the classic and alternative bile acid synthesis pathway, bile acid composition and bile acid pool size, and intestinal bile acid signaling and gut microbiome in regulation of bile acid homeostasis.


Synthesis ◽  
2021 ◽  
Author(s):  
Leonid Fershtat ◽  
Fedor Teslenko

Five-membered heterocyclic N-oxides attracted special attention due to their strong application potential in medicinal chemistry and advanced materials science. In this regard, novel methods for their synthesis and functionalization are constantly required. In this short review, recent state-of-the-art achievements in the chemistry of isoxazoline N-oxides, 1,2,3-triazole 1-oxides and 1,2,5-oxadiazole 2-oxides are briefly summarized. Main routes to transition-metal-catalyzed and metal-free functionalization protocols along with mechanistic considerations are outlined. Transformation patterns of the hetarene N-oxide rings as precursors to other nitrogen heterocyclic systems are also presented.


2018 ◽  
Vol 61 (24) ◽  
pp. 10935-10956 ◽  
Author(s):  
Bahaa El-Dien M. El-Gendy ◽  
Shaimaa S. Goher ◽  
Lamees S. Hegazy ◽  
Mohamed M. H. Arief ◽  
Thomas P. Burris

2019 ◽  
Vol 17 (31) ◽  
pp. 7270-7292 ◽  
Author(s):  
Sagar S. Thorat ◽  
Ravindar Kontham

Oxaspirolactones are ubiquitous structural motifs found in natural products and synthetic molecules with a diverse biochemical and physicochemical profile, and represent a valuable target in natural product chemistry and medicinal chemistry.


2020 ◽  
Vol 37 (11) ◽  
pp. 1511-1531
Author(s):  
Zhi-Chen Wu ◽  
Dale L. Boger

This review summarizes and highlights recent advances in medicinal chemistry of natural products enabled by total synthesis that provide “supernatural products” with improved properties superseding the natural products themselves.


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