Bioorganic & Medicinal Chemistry Letters 2010-02-15

Synthesis and structure-activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists.

Brian W Budzik, Karen A Evans, David D Wisnoski, Jian Jin, Ralph A Rivero, George R Szewczyk, Channa Jayawickreme, David L Moncol, Hongshi Yu

文献索引：Bioorg. Med. Chem. Lett. 20(4) , 1363-7, (2010)

全文：HTML全文

摘要

A series of 3-aryl-4-isoxazolecarboxamides identified from a high-throughput screening campaign as novel, potent agonists of the human TGR5 G-protein-coupled receptor is described. Many analogues were readily accessible via solution-phase synthesis which resulted in the rapid identification of key structure-activity relationships (SAR), and the discovery of potent exemplars (up to pEC50=9). Details of the SAR and optimization of this series are presented herein.Copyright 2010 Elsevier Ltd. All rights reserved.

相关化合物

  • 4-氯-N-甲基苯胺

相关文献：

The role of pharmacokinetics and metabolism in species sensitivity to neurotoxic agents.

1986-02-01

[Fundam. Appl. Toxicol. 6(2) , 190-207, (1986)]

FT-IR, FT-Raman, NMR spectra and DFT calculations on 4-chloro-N-methylaniline.

2010-05-01

[Spectrochim. Acta. A. Mol. Biomol. Spectrosc. 75(5) , 1523-9, (2010)]

Inhibition of hepatic drug metabolism in VX2 carcinoma-bearing rabbits.

1980-01-01

[Drug Metab. Dispos. 8(3) , 139-42, (1980)]

Effect of dietary malathion on hepatic microsomal drug-metabolizing systems of Gallus domesticus.

1986-05-01

[Toxicol. Lett. 31(2) , 107-11, (1986)]

Studies on the cytochrome P-450 of avocado (Persea [corrected] americana) mesocarp microsomal fraction.

1990-07-01

[Xenobiotica 20(7) , 711-26, (1990)]

更多文献...