4.7 Article

Design, synthesis and biological evaluation of novel indole derivatives as gut-selective NaPi2b inhibitors

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Chemistry, Medicinal

Discovery of Gut-Restricted Small-Molecule Inhibitors of Intestinal Sodium-Dependent Phosphate Transport Protein 2b (NaPi2b) for the Treatment of Hyperphosphatemia

Michihiro Maemoto et al.

Summary: NaPi2b is expressed in the small intestine, lungs, and testes and plays a vital role in phosphate homeostasis. Inhibiting NaPi2b can reduce phosphate absorption, making it a potential treatment for hyperphosphatemia. Compound 15, a zwitterionic compound, has shown strong in vitro inhibitory activity and low membrane permeability.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of novel 1H-pyrazole-4-carbo-nyl-4,5,6,7-tetrahydrobenzo [b]thiophene derivatives as gut-selective NaPi2b inhibitors

Yasunobu Ushiki et al.

Summary: Inhibitors of intestinal sodium-dependent phosphate transport protein 2b have potential as new anti-hyperphosphatemia drug candidates. Two synthesized compounds, 36a and 36b, showed good in vitro activity and low bioavailability in Sprague-Dawley rats. However, these compounds failed to suppress phosphate absorption in vivo.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2022)

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of novel pyridine derivatives as gut-selective NaPi2b inhibitors

Yasunobu Ushiki et al.

Summary: A novel gut-selective NaPi2b inhibitor with good activity in vitro and relatively low hydrophobicity was identified in this study. The compound demonstrated the ability to suppress phosphate absorption in vivo.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2022)

Article Urology & Nephrology

NPT-IIb Inhibition Does Not Improve Hyperphosphatemia in CKD

Tobias E. Larsson et al.

KIDNEY INTERNATIONAL REPORTS (2018)

Article Chemistry, Medicinal

A Survey of the Role of Noncovalent Sulfur Interactions in Drug Design

Brett R. Beno et al.

JOURNAL OF MEDICINAL CHEMISTRY (2015)

Article Chemistry, Multidisciplinary

Cell-Permeable Cyclic Peptides from Synthetic Libraries Inspired by Natural Products

William M. Hewitt et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2015)

Review Respiratory System

Pulmonary alveolar microlithiasis: review of the 1022 cases reported worldwide

Giuseppe Castellana et al.

EUROPEAN RESPIRATORY REVIEW (2015)

Review Urology & Nephrology

The role of the gastrointestinal tract in phosphate homeostasis in health and chronic kidney disease

Joanne Marks et al.

CURRENT OPINION IN NEPHROLOGY AND HYPERTENSION (2013)

Article Urology & Nephrology

Intestinal Npt2b Plays a Major Role in Phosphate Absorption and Homeostasis

Yves Sabbagh et al.

JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY (2009)

Article Pharmacology & Pharmacy

Measurements of rat and mouse gastrointestinal pH fluid and lymphoid tissue, and implications for in-vivo experiments

Emma L. McConnell et al.

JOURNAL OF PHARMACY AND PHARMACOLOGY (2008)

Article Critical Care Medicine

Mutations in the SLC34A2 gene are associated with pulmonary alveolar microlithiasis

Huqun et al.

AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE (2007)

Article Chemistry, Medicinal

Molecular properties that influence the oral bioavailability of drug candidates

DF Veber et al.

JOURNAL OF MEDICINAL CHEMISTRY (2002)