Recent progress on bile acid receptor modulators for treatment of metabolic diseases

Y Xu - Journal of medicinal chemistry, 2016 - ACS Publications
Bile acids are steroid-derived molecules synthesized in the liver, secreted from hepatocytes
into the bile canaliculi, and subsequently stored in the gall bladder. During the feeding, bile …

Highly modular flow cell for electroorganic synthesis

C Gütz, A Stenglein… - Organic Process Research …, 2017 - ACS Publications
A highly modular electrochemical flow cell and its application in electroorganic synthesis is
reported. This innovative setup facilitates many aspects: an easy adjustment of electrode …

Chemistry and pharmacology of GPBAR1 and FXR selective agonists, dual agonists, and antagonists

S De Marino, C Festa, V Sepe, A Zampella - Bile Acids and Their …, 2019 - Springer
In the recent years, bile acid receptors FXR and GPBAR1 have attracted the interest of
scientific community and companies, as they proved promising targets for the treatment of …

[HTML][HTML] Design, synthesis and bioactivity of myricetin derivatives for control of fungal disease and tobacco mosaic virus disease

X Cao, B He, F Liu, Y Zhang, L Xing, N Zhang, Y Zhou… - RSC …, 2023 - pubs.rsc.org
A series of myricetin derivatives containing isoxazole were designed and synthesized. All
the synthesized compounds were characterized by NMR and HRMS. In terms of antifungal …

Hit-to-Lead Optimization of Heterocyclic Carbonyloxycarboximidamides as Selective Antagonists at Human Adenosine A3 Receptor

X Huang, A Chorianopoulou, P Kalkounou… - Journal of Medicinal …, 2024 - ACS Publications
Antagonism of the human adenosine A3 receptor (hA3R) has potential therapeutic
application. Alchemical relative binding free energy calculations of K18 and K32 suggested …

[HTML][HTML] Reagent-controlled regiodivergent intermolecular cyclization of 2-aminobenzothiazoles with β-ketoesters and β-ketoamides

II Roslan, KH Ng, GK Chuah… - Beilstein Journal of …, 2017 - beilstein-journals.org
Two regiodivergent approaches to intermolecular cyclization of 2-aminobenzothiazoles with
β-ketoesters and amides have been developed, controlled by the reagents employed. With …

Pyrazolyl Thioureas and Carbothioamides with an NNSN Motif against MSSA and MRSA

A Delpe-Acharige, M Zhang, K Eschliman, A Dalecki… - ACS …, 2021 - ACS Publications
A novel series of copper-activatable drugs intended for use against methicillin-sensitive
Staphylococcus aureus (MSSA) and methicillin-resistant S. aureus (MRSA) were …

Novel chemoenzymatic oxidation of amines into oximes based on hydrolase-catalysed peracid formation

D Méndez-Sánchez, I Lavandera, V Gotor… - Organic & …, 2017 - pubs.rsc.org
The efficient transformation of benzylamines into the corresponding oximes has been
described by means of a chemoenzymatic process. This strategy is based on a two-step …

Discovery of isatin and 1H-indazol-3-ol derivatives as d-amino acid oxidase (DAAO) inhibitors

B Szilágyi, P Kovács, GG Ferenczy, A Rácz… - Bioorganic & Medicinal …, 2018 - Elsevier
Abstract d-Amino acid oxidase (DAAO) is a potential target in the treatment of schizophrenia
as its inhibition increases brain d-serine level and thus contributes to NMDA receptor …

[3+ 2] cycloaddition of 1-(4-Methoxybenzyl) indoles and azaindoles with nitrile oxides

R Kimura, Y Sato, K Morisaki, T Nishi - Tetrahedron, 2022 - Elsevier
Abstract We studied [3+ 2] cycloaddition reactions of indoles and azaindoles with various
nitrile oxides. N-Protection of indoles and azaindoles with the 4-methoxybenzyl group was …