✦ LIBER ✦

A Novel Series of 2-Carboxytetrahydroquinolines Provides New Insights into the Eastern Region of Glycine Site NMDA Antagonists

✍ Scribed by Gerd Dannhardt; Markus v. Gruchalla; Beate K. Kohl; C. G. Parsons

Book ID: 101386781
Publisher: John Wiley and Sons
Year: 2000
Tongue: English
Weight: 96 KB
Volume: 333
Category: Article
ISSN: 0365-6233
DOI: 10.1002/1521-4184(20008)333:8<267::aid-ardp267>3.0.co;2-0

No coin nor oath required. For personal study only.

✦ Synopsis

A series of potent 4-substituted tetrahydroquinolines has been synthesized and biologically tested in order to refine the eastern region of the pharmacophore model for glycine site NMDA antagonists concerning the assessment of lipophilicity, flexibility, and hydrogen bonding. Displacement studies on rat cortical membranes using [3H]-5,7-dichlorokynurenic acid as a radioligand indicated that binding affinities are markedly enhanced when additional hydrogen-accepting groups are introduced into the eastern region of the 2-carboxytetrahydroquinolines. Among the most potent ligands were some urea, sulfonylurea, and crown ether compounds as interesting leads for new diagnostics, especially for the evaluation of PET tracers, which allow biodistribution studies and NMDA receptor studies in the living organism.

📜 SIMILAR VOLUMES

ChemInform Abstract: A Series of Quinoli

ChemInform Abstract: A Series of Quinoline-2-carboxylic Acid Derivatives: New Potent Glycine Site NMDA Receptor Antagonists.

✍ R. H. KIM; J. I. CHOI; S. W. CHOI; K. S. LEE; Y. S. JUNG; W. K. PARK; C. M. SEON 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 30 KB 👁 2 views

## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable v

Indeno[1,2- b ]pyrazin-2,3-diones: A New

Indeno[1,2- b ]pyrazin-2,3-diones: A New Class of Antagonists at the Glycine Site of the NMDA Receptor with Potent in Vivo Activity

✍ Jimonet, Patrick; Ribeill, Yves; Bohme, Georg Andrees; Boireau, Alain; Chevé,, M 📂 Article 📅 2000 🏛 American Chemical Society 🌐 English ⚖ 233 KB

ChemInform Abstract: Indeno[1,2-b]pyrazi

ChemInform Abstract: Indeno[1,2-b]pyrazine-2,3-diones: A New Class of Antagonists at the Glycine Site of the NMDA Receptor with Potent in vivo Activity.

✍ Patrick Jimonet; et al. et al. 📂 Article 📅 2000 🏛 John Wiley and Sons ⚖ 29 KB 👁 2 views

A New Series of Highly Potent Non-Peptid

A New Series of Highly Potent Non-Peptide Bradykinin B 2 Receptor Antagonists Incorporating the 4-Heteroarylquinoline Framework. Improvement of Aqueous Solubility and New Insights into Species Difference

✍ Sawada, Yuki; Kayakiri, Hiroshi; Abe, Yoshito; Imai, Keisuke; Mizutani, Tsuyoshi 📂 Article 📅 2004 🏛 American Chemical Society 🌐 English ⚖ 302 KB

4-[(Carboxymethyl)oxy]- and 4-[(carboxym

4-[(Carboxymethyl)oxy]- and 4-[(carboxymethyl)amino]-5,7-dichloroquinoline-2-carboxylic acid: new antagonists of the strychnine-insensitive glycine binding site on the N-methyl-D-aspartate (NMDA) receptor complex

✍ Harrison, Boyd L.; Baron, Bruce M.; Cousino, Diane M.; McDonald, Ian A. 📂 Article 📅 1990 🏛 American Chemical Society 🌐 English ⚖ 425 KB