𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Synthesis and structure–Activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists

✍ Scribed by Zhiqiang Guo; Yongsheng Chen; Dongpei Wu; Yun-Fei Zhu; R.Scott Struthers; John Saunders; Qiu Xie; Chen Chen

Book ID
104364064
Publisher
Elsevier Science
Year
2003
Tongue
English
Weight
221 KB
Volume
13
Category
Article
ISSN
0960-894X

No coin nor oath required. For personal study only.

✦ Synopsis

The synthesis and SAR studies of thieno [2,3-d]pyrimidine-2,4-diones as human GnRH receptor antagonists to treat reproductive diseases are discussed. It was found that the 2-(2-pyridyl)ethyl group on the 5-aminomethyl functionality of the core structure was a key feature for good receptor binding activity. SAR study of the 6-(4-aminophenyl) group suggests that hydrophobic substituents were preferred. The best compound from this series had binding affinity (K i ) of 0.4 nM to the human GnRH receptor.

📜 SIMILAR VOLUMES

ChemInform Abstract: A Novel Synthesis o
ChemInform Abstract: A Novel Synthesis of 2-Arylpyrrolo[1,2-a]pyrimid-7-ones and Their Structure—Activity Relationships as Potent GnRH Receptor Antagonists.
✍ Yun-Fei Zhu; Chen Chen; et al. et al. 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 35 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

Synthesis and Structure—Activity Relatio
Synthesis and Structure—Activity Relationships of 3H-Quinazolin-4-ones and 3H-Pyrido[2,3-d]pyrimidin-4-ones as CXCR3 Receptor Antagonists.
✍ Stefania Storelli; Dennis Verzijl; Jawad Al-Badie; Niels Elders; Leontien Bosch; 📂 Article 📅 2007 🏛 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 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.