Phenyl bioisosteres in medicinal chemistry: discovery of novel γ-secretase modulators as a potential treatment for Alzheimer's disease

文献情報

出版日 2021-04-12

DOI 10.1039/D1MD00043H

インパクトファクター 0

著者

H. Ratni, K. Baumann, P. Bellotti, X. A. Cook, L. G. Green, T. Luebbers, M. Reutlinger, A. F. Stepan, W. Vifian

原文を見る

要旨

Phenyl rings are one of the most prevalent structural moieties in active pharmaceutical ingredients, even if they often contribute to poor physico-chemical properties. Herein, we propose the use of a bridged piperidine (BP) moiety as a phenyl bioisostere, which could also be seen as a superior phenyl alternative as it led to strongly improved drug like properties, in terms of solubility and lipophilicity. Additionally, this BP moiety compares favorably to the recently reported saturated phenyl bioisosteres. We applied this concept to our γ-secretase modulator (GSM) project for the potential treatment of Alzheimer's disease delivering clinical candidates.

掲載誌

RSC Medicinal Chemistry

CiteScore: 0

自己引用率: 0%

年間論文数: 0

Phenyl bioisosteres in medicinal chemistry: discovery of novel γ-secretase modulators as a potential treatment for Alzheimer's disease

文献情報

おすすめジャーナル

関連文献

Addressing the practicalities of anodic stripping voltammetry for heavy metal detection: a tutorial review

A novel logic gate based on liquid-crystals responding to the DNA conformational transition

Mass spectrometric analysis of PTM dynamics using stable isotope labeled metabolic precursors in cell culture

Enzymatic reaction-based nanopore detection of zinc ions

Screening of DNA G-quadruplex stabilizing ligands by nano differential scanning fluorimetry

Emerging paper microfluidic devices

Development of portable defocusing micro-scale spatially offset Raman spectroscopy

pulSED: pulsed sonoelectrodeposition of fractal nanoplatinum for enhancing amperometric biosensor performance

A two-photon fluorescent probe for bio-imaging of formaldehyde in living cells and tissues

A one-step colorimetric acid–base titration sensor using a complementary color changing coordination system

こちらもおすすめ

カルボニル基が付いた5-氰基-1-{[(2-メチル-2-プロpanyl)オキシ]カーボンイル}1H-吲哚-2-イリド-2-ボリン酸はどのように保存すればよいですか？

tert-ブチル2-クロロメチルピリジン-3-基炭酸エステルの市場動向や研究トレンドはどうですか？

聚二季戊四醇六丙烯酸酯はどの業界で使用されていますか？

1-氯-5-硝基异喹啉の市場動向や研究トレンドはどうですか？

2-チロール-5-メチルスルフェニル-3-trifルオルメチルベンゼンはどのように合成されますか？

p-トールイルマグネシウムブロミドの物理化学的性質は何ですか？

1-(5-甲基-2-硫化素基)プロパン-1-酮の市場動向や研究トレンドはどうですか？

十一碳烯酰甘氨酸を取り扱う際の実験室安全事項は何ですか？

1H,1H-全氟-3,6-二氧杂葵-1-醇を取り扱う際の実験室安全事項は何ですか？

3-(4-(フルオロメチルオキシ)フェニル)-1,2,4-オキサジアゾール-5-カルボハイドライドは安全ですか？

掲載誌

RSC Medicinal Chemistry

おすすめ化合物

tert-Butyl 4-chloro-5-methoxypyridin-3-ylcarbamate

4-{[4-(Trifluoromethoxy)benzyl]oxy}benzonitrile

N~2~,2-Dimethyl-1,2-propanediamine

2-Methylbenzene-1,3,5-triamine trihydrochloride

2-Methyl-4-(trifluoromethoxy)benzoic acid

おすすめサプライヤー